Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ligand		 Fold
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GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

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weight		 Rot
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 DOI
11583188 146060 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
CHEMBL379125 146060 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
44400674 131967 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 131967 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
17449900 146320 13 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 146320 13 None -2 3 Human 9.2 pEC50 = 9.2 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
16094675 88932 1 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.3 Cc1cccc(NC(=O)CN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
CHEMBL216922 88932 1 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.3 Cc1cccc(NC(=O)CN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
10359019 90100 5 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3ccccc3F)CC2)c1 10.1021/jm060662k
CHEMBL219129 90100 5 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3ccccc3F)CC2)c1 10.1021/jm060662k
10088259 108690 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
CHEMBL300956 108690 3 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
44400585 75430 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 75430 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
2 10035 23 None -2 6 Human 8.9 pEC50 = 8.9 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
54562 10035 23 None -2 6 Human 8.9 pEC50 = 8.9 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
CHEMBL240773 10035 23 None -2 6 Human 8.9 pEC50 = 8.9 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
11725531 60828 2 None - 1 Human 8.8 pEC50 = 8.8 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160626 60828 2 None - 1 Human 8.8 pEC50 = 8.8 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
6469918 86666 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 86666 13 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
681 8247 72 None -7 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 8247 72 None -7 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 8247 72 None -7 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 8247 72 None -7 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 8247 72 None -7 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
155559617 181663 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 181663 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
44400585 75430 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 75430 0 None 2 2 Human 8.7 pEC50 = 8.7 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
10378194 204544 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL57176 204544 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
681 8247 72 None -7 14 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
940 8247 72 None -7 14 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
947 8247 72 None -7 14 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
CHEMBL59 8247 72 None -7 14 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
DB00988 8247 72 None -7 14 Human 8.0 pEC50 = 8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
10383724 90186 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 5 1 4 2.9 CSc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219570 90186 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 5 1 4 2.9 CSc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
16094681 90122 0 None -1 2 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219261 90122 0 None -1 2 Rat 7.0 pEC50 = 7 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
16094684 143378 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 347 4 1 3 2.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1F 10.1021/jm060662k
CHEMBL373964 143378 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 347 4 1 3 2.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1F 10.1021/jm060662k
10065188 108381 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
CHEMBL298763 108381 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
155568867 182933 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 182933 0 None -3 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
11221906 86686 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
CHEMBL212444 86686 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
155536720 178966 0 None 37 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 178966 0 None 37 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
11849262 86892 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 337 7 0 4 3.6 CCO/N=C(\CCN1CCN(c2ccccc2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213246 86892 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 337 7 0 4 3.6 CCO/N=C(\CCN1CCN(c2ccccc2)CC1)c1ccccc1 10.1021/jm060279f
2 10035 23 None -2 6 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
54562 10035 23 None -2 6 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
CHEMBL240773 10035 23 None -2 6 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
11849223 86622 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL212189 86622 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
25142456 89181 2 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 89181 2 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
44418745 90185 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 3.8 CCc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL219567 90185 1 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 3.8 CCc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
11325818 86563 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL211930 86563 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
10428669 90240 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 361 4 1 3 3.0 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc2ccccc2c1 10.1021/jm060662k
CHEMBL220015 90240 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 361 4 1 3 3.0 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc2ccccc2c1 10.1021/jm060662k
9835713 25258 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL127226 25258 1 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
10404144 212081 23 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL7927 212081 23 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
10361512 61213 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160932 61213 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Tested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assayTested for the effective concentration against human D4.2 receptor in CHO 10001 cells established in mitogenesis assay
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
168285560 199697 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 199697 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 199697 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
5025739 175975 45 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL440687 175975 45 None -1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
44414898 145684 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 341 6 1 7 1.0 CO/N=C(/c1cccnc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL378302 145684 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 341 6 1 7 1.0 CO/N=C(/c1cccnc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
10316440 148444 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 3.1 Cc1ccc(Cl)cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL385417 148444 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 3.1 Cc1ccc(Cl)cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
16094706 148687 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 346 4 1 4 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cnccc1Cl 10.1021/jm060662k
CHEMBL386917 148687 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 346 4 1 4 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cnccc1Cl 10.1021/jm060662k
10382581 108075 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
CHEMBL296506 108075 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
44400626 77177 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 77177 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
11849638 86789 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL212847 86789 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
11772242 173066 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL427048 173066 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
9861462 90109 0 None -5 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL219179 90109 0 None -5 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
5025739 175975 45 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL440687 175975 45 None -1 3 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
16094682 90254 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 370 5 1 5 2.4 Cc1ccc([N+](=O)[O-])cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL220139 90254 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 370 5 1 5 2.4 Cc1ccc([N+](=O)[O-])cc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
11280225 87871 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
CHEMBL215569 87871 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
10430781 90053 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 395 5 1 4 3.0 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(OC(F)(F)F)c1 10.1021/jm060662k
CHEMBL218852 90053 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 395 5 1 4 3.0 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(OC(F)(F)F)c1 10.1021/jm060662k
11849734 86927 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 363 7 0 6 2.9 CCO/N=C(\CCN1CCN(c2ncccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213398 86927 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 363 7 0 6 2.9 CCO/N=C(\CCN1CCN(c2ncccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
10425450 6989 30 None 125 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
3301 6989 30 None 125 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
CHEMBL375596 6989 30 None 125 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
44400519 139907 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 139907 0 None -2 2 Human 7.9 pEC50 = 7.9 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
681 8247 72 None -7 14 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
940 8247 72 None -7 14 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
947 8247 72 None -7 14 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
CHEMBL59 8247 72 None -7 14 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
DB00988 8247 72 None -7 14 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
16094672 90044 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 4.9 O=C(CN1CCC(c2ccccn2)CC1)Nc1c(Cl)cc(Cl)cc1Cl 10.1021/jm060662k
CHEMBL218797 90044 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 4.9 O=C(CN1CCC(c2ccccn2)CC1)Nc1c(Cl)cc(Cl)cc1Cl 10.1021/jm060662k
11451703 145796 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
CHEMBL378576 145796 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
10642239 193438 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL48819 193438 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
119570 9933 96 None -4 10 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2233 9933 96 None -4 10 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
953 9933 96 None -4 10 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
CHEMBL301265 9933 96 None -4 10 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
DB00413 9933 96 None -4 10 Human 7.8 pEC50 = 7.8 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
16094666 88502 3 None 251 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 88502 3 None 251 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
10022369 90263 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 375 5 1 4 2.5 COc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
CHEMBL220192 90263 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 375 5 1 4 2.5 COc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
10665101 108302 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
CHEMBL298166 108302 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
10404144 212081 23 None - 1 Human 7.8 pEC50 = 7.8 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL7927 212081 23 None - 1 Human 7.8 pEC50 = 7.8 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
168268756 199543 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 199543 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 199543 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
16094678 90160 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(F)c1 10.1021/jm060662k
CHEMBL219417 90160 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(F)c1 10.1021/jm060662k
10045314 172762 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cc(Cl)cc(Cl)c1 10.1021/jm060662k
CHEMBL425288 172762 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cc(Cl)cc(Cl)c1 10.1021/jm060662k
11175610 144903 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.4 CC(C)O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL376639 144903 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.4 CC(C)O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
6603820 102549 19 None -1 7 Human 7.8 pEC50 = 7.8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
CHEMBL25856 102549 19 None -1 7 Human 7.8 pEC50 = 7.8 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
3645619 9808 20 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
975 9808 20 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
CHEMBL45244 9808 20 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
1353 8692 93 None -3 39 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
3559 8692 93 None -3 39 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
86 8692 93 None -3 39 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
CHEMBL54 8692 93 None -3 39 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
DB00502 8692 93 None -3 39 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(03)00587-0
11849636 86621 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL212188 86621 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
11849225 86954 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL213518 86954 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
16094666 88502 3 None 251 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/jm060662k
CHEMBL216393 88502 3 None 251 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/jm060662k
16094705 90139 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 429 5 1 4 3.4 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(OC(F)(F)F)c(Cl)c1 10.1021/jm060662k
CHEMBL219340 90139 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 429 5 1 4 3.4 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(OC(F)(F)F)c(Cl)c1 10.1021/jm060662k
11325645 145455 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
CHEMBL377794 145455 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
44415054 87904 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N\O)c2ccccc2)CC1 10.1021/jm060279f
CHEMBL215670 87904 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N\O)c2ccccc2)CC1 10.1021/jm060279f
9997550 143377 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
CHEMBL373963 143377 1 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
10339711 90182 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1Cl 10.1021/jm060662k
CHEMBL219564 90182 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.4 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1Cl 10.1021/jm060662k
11849777 145410 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
CHEMBL377585 145410 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
2 10035 23 None -2 6 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
54562 10035 23 None -2 6 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
CHEMBL240773 10035 23 None -2 6 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
135407844 86859 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 2.5 Cc1ccc(O)c(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL213106 86859 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 2.5 Cc1ccc(O)c(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
11849639 87132 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL214343 87132 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
11849816 84854 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL210101 84854 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
11849822 86884 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(\c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
CHEMBL213208 86884 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(\c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
2 10035 23 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00814-9
54562 10035 23 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00814-9
CHEMBL240773 10035 23 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00814-9
2 10035 23 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
54562 10035 23 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
CHEMBL240773 10035 23 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
681 8247 72 None -7 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
940 8247 72 None -7 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
947 8247 72 None -7 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
CHEMBL59 8247 72 None -7 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
DB00988 8247 72 None -7 14 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
2 10035 23 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(02)00316-5
54562 10035 23 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(02)00316-5
CHEMBL240773 10035 23 None -2 6 Human 8.7 pEC50 = 8.7 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(02)00316-5
11849637 86648 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL212298 86648 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1cccc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
9861462 90109 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL219179 90109 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
681 8247 72 None -1 14 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
940 8247 72 None -1 14 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
947 8247 72 None -1 14 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
CHEMBL59 8247 72 None -1 14 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
DB00988 8247 72 None -1 14 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm060662k
44400674 131967 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 131967 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
6469918 86666 13 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 86666 13 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
2 10035 23 None -2 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
54562 10035 23 None -2 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
CHEMBL240773 10035 23 None -2 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assayAgonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acsmedchemlett.9b00050
10425450 6989 30 None 125 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 6989 30 None 125 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 6989 30 None 125 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
11439072 175738 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N/O)c2ccccc2)CC1 10.1021/jm060279f
CHEMBL438961 175738 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 335 5 1 6 2.3 N#Cc1cccnc1N1CCN(CC/C(=N/O)c2ccccc2)CC1 10.1021/jm060279f
11849635 87154 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N\O 10.1021/jm060279f
CHEMBL214440 87154 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N\O 10.1021/jm060279f
681 8247 72 None -7 14 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
940 8247 72 None -7 14 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
947 8247 72 None -7 14 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
CHEMBL59 8247 72 None -7 14 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
DB00988 8247 72 None -7 14 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
11849182 86644 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL212288 86644 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
16094698 144646 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
CHEMBL376092 144646 4 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
44417647 88936 0 None 52 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL1203924 88936 0 None 52 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL216945 88936 0 None 52 3 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
11301354 148426 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL385350 148426 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
10617381 196465 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
CHEMBL51536 196465 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
44400553 77554 0 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 77554 0 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
11849821 176079 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL441529 176079 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
44400553 77554 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 77554 0 None -2 2 Human 7.6 pEC50 = 7.6 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL None None None None 10.1021/jm050170s
2 10035 23 None -2 6 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
54562 10035 23 None -2 6 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
CHEMBL240773 10035 23 None -2 6 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2006.02.075
24878061 148189 0 None 4 2 Human 6.6 pEC50 = 6.6 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
CHEMBL384046 148189 0 None 4 2 Human 6.6 pEC50 = 6.6 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
11849633 87353 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL214954 87353 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
9883554 172133 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL423659 172133 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
11163137 148515 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL385826 148515 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094671 90152 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 4 1 3 4.2 Cc1cc(Cl)cc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL219392 90152 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 357 4 1 3 4.2 Cc1cc(Cl)cc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
10338536 88909 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 2.8 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
CHEMBL216721 88909 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 359 4 1 3 2.8 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1Cl 10.1021/jm060662k
11269392 84785 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
CHEMBL209759 84785 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
11849634 148401 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL385230 148401 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
11849265 146318 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.3 CCO/N=C(\CCN1CCN(c2ncccc2C)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL379597 146318 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 7 0 5 3.3 CCO/N=C(\CCN1CCN(c2ncccc2C)CC1)c1ccccc1 10.1021/jm060279f
11738945 86722 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(/CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212595 86722 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(/CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
2653640 72993 12 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
CHEMBL184486 72993 12 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
11849263 167716 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2cccc(OC)c2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL411545 167716 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2cccc(OC)c2)CC1)c1ccccc1 10.1021/jm060279f
681 8247 72 None -7 14 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
940 8247 72 None -7 14 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
947 8247 72 None -7 14 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
CHEMBL59 8247 72 None -7 14 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
DB00988 8247 72 None -7 14 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.2c00840
3303 9024 46 None 1 5 Human 7.6 pEC50 = 7.6 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
5311200 9024 46 None 1 5 Human 7.6 pEC50 = 7.6 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
CHEMBL267014 9024 46 None 1 5 Human 7.6 pEC50 = 7.6 Functional
Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assayTested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
11849776 86547 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
CHEMBL211836 86547 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
11739255 86793 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212861 86793 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
10042205 143724 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccccc1F 10.1021/jm060662k
CHEMBL374326 143724 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccccc1F 10.1021/jm060662k
11256262 86776 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212782 86776 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
45361874 176800 2 None 58 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 176800 2 None 58 3 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11474734 86700 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(/c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
CHEMBL212490 86700 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 388 7 0 6 2.9 CO/N=C(/c1ccc(Cl)cc1)C(CN1CCN(c2ccccn2)CC1)OC 10.1021/jm060279f
16094685 90406 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 317 4 1 3 1.9 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)NC1CCCCC1 10.1021/jm060662k
CHEMBL220469 90406 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 317 4 1 3 1.9 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)NC1CCCCC1 10.1021/jm060662k
11292299 86545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
CHEMBL211829 86545 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1Cl 10.1021/jm060279f
6469693 86730 17 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 86730 17 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assayActivity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
10593191 195887 1 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
CHEMBL51023 195887 1 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
6466372 176841 12 None 58 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 176841 12 None 58 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
4797946 177203 7 None 81 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 177203 7 None 81 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
16094704 88931 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 2 4 2.9 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cn3)CC2)c1 10.1021/jm060662k
CHEMBL216921 88931 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 2 4 2.9 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cn3)CC2)c1 10.1021/jm060662k
11849224 86808 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212902 86808 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 1 5 2.6 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
10616050 193425 3 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL48807 193425 3 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
2 10035 23 None -2 6 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
54562 10035 23 None -2 6 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
CHEMBL240773 10035 23 None -2 6 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
10247720 19826 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 19826 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 19826 1 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesisAgonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
10018402 88908 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 312 4 1 4 1.3 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccn1 10.1021/jm060662k
CHEMBL216719 88908 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 312 4 1 4 1.3 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccn1 10.1021/jm060662k
11324794 145037 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377050 145037 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094677 90111 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219185 90111 0 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11198974 86785 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 8 0 5 3.4 CCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212831 86785 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 8 0 5 3.4 CCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
11849299 86170 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 430 9 0 6 3.9 CO/N=C(/c1ccc(Cl)cc1)C(COC(C)C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL211360 86170 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 430 9 0 6 3.9 CO/N=C(/c1ccc(Cl)cc1)C(COC(C)C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
10405923 90178 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 6 1 4 2.3 CCOc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219551 90178 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 6 1 4 2.3 CCOc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11849229 144952 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL376955 144952 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
11370781 86646 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
CHEMBL212291 86646 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
11849820 84729 0 None 10 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL209645 84729 0 None 10 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11849267 86647 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212292 86647 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
11849730 86724 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2ccccc2OC)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212607 86724 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 367 8 0 5 3.6 CCO/N=C(\CCN1CCN(c2ccccc2OC)CC1)c1ccccc1 10.1021/jm060279f
11849180 86583 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N\O)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212028 86583 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N\O)c1cccc(C)c1 10.1021/jm060279f
16094668 90101 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 322 4 1 2 4.1 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C)CC2)c1 10.1021/jm060662k
CHEMBL219130 90101 3 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 322 4 1 2 4.1 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C)CC2)c1 10.1021/jm060662k
10405922 90183 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.5 COc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219565 90183 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.5 COc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
11849780 86958 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
CHEMBL213558 86958 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
16094683 144651 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.8 Cc1ccc(Cl)c(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1Cl 10.1021/jm060662k
CHEMBL376196 144651 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.8 Cc1ccc(Cl)c(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1Cl 10.1021/jm060662k
10042826 172918 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL426167 172918 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cccc(C)c1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
44415055 87916 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 381 9 0 5 4.0 CCO/N=C(\CCN1CCN(c2cccc(OCC)c2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL215704 87916 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 381 9 0 5 4.0 CCO/N=C(\CCN1CCN(c2cccc(OCC)c2)CC1)c1ccccc1 10.1021/jm060279f
155530763 178348 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 178348 0 None -2 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
44400519 139907 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 139907 0 None -2 2 Human 7.5 pEC50 = 7.5 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
11849684 86990 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 350 8 0 5 3.2 C=CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213700 86990 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 350 8 0 5 3.2 C=CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094674 148445 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 3.1 Cc1cccc(NC(=O)CN2CCC(c3cccc(C#N)n3)CC2)c1 10.1021/jm060662k
CHEMBL385418 148445 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 3.1 Cc1cccc(NC(=O)CN2CCC(c3cccc(C#N)n3)CC2)c1 10.1021/jm060662k
16094708 172852 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 387 5 1 3 3.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(-c2ccccc2)c1 10.1021/jm060662k
CHEMBL425793 172852 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 387 5 1 3 3.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(-c2ccccc2)c1 10.1021/jm060662k
11164276 86527 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL211732 86527 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
11199162 86634 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212235 86634 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
10404935 90184 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C 10.1021/jm060662k
CHEMBL219566 90184 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C 10.1021/jm060662k
11849228 103191 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 366 9 0 5 3.8 CCCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL261957 103191 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 366 9 0 5 3.8 CCCCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
11151081 86570 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL211972 86570 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
11849222 87994 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N/O 10.1021/jm060279f
CHEMBL215849 87994 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 324 5 1 5 2.8 Cc1ccccc1/C(CCN1CCN(c2ccccn2)CC1)=N/O 10.1021/jm060279f
228 7233 28 None -1 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 7233 28 None -1 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 7233 28 None -1 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 7233 28 None -1 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 7233 28 None -1 19 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
11185987 87123 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL214314 87123 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
6469693 86730 17 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 86730 17 None - 1 Human 8.4 pEC50 = 8.4 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
11849179 87920 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N/O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
CHEMBL215723 87920 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N/O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
44418748 177238 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 4 3.2 COc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL444881 177238 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 4 3.2 COc1cccc(C)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
11450607 86947 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
CHEMBL213486 86947 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
155552185 180840 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 180840 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
11849819 87021 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL213828 87021 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 356 7 0 5 3.2 CO/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11371795 86595 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL212073 86595 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
10472323 90034 4 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.8 COc1ccccc1C1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1021/jm060662k
CHEMBL218761 90034 4 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 338 5 1 3 3.8 COc1ccccc1C1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1021/jm060662k
11849817 145708 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 314 4 1 5 2.2 O/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL378427 145708 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 314 4 1 5 2.2 O/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11771801 86804 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212891 86804 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
10084583 111555 4 None -151 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 111555 4 None -151 3 Human 6.4 pEC50 = 6.4 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
11849775 172975 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL426510 172975 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
11849823 86380 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N\O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
CHEMBL211463 86380 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 340 5 2 6 1.8 Cc1cccc(/C(=N\O)C(O)CN2CCN(c3ccccn3)CC2)c1 10.1021/jm060279f
11151919 86961 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL213572 86961 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 7 0 5 3.0 CCO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
10385089 148508 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cc(Cl)cc(Cl)c1 10.1021/jm060662k
CHEMBL385781 148508 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1cc(Cl)cc(Cl)c1 10.1021/jm060662k
11849681 86576 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 5 1 5 3.1 Cc1cc(C)cc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
CHEMBL211985 86576 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 5 1 5 3.1 Cc1cc(C)cc(/C(CCN2CCN(c3ccccn3)CC2)=N/O)c1 10.1021/jm060279f
11849181 86835 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL213004 86835 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
11211058 87109 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL214247 87109 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
11187957 146308 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(/CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL379546 146308 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(/CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
11849778 87917 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL215705 87917 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
16094709 90110 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 3.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1C(F)(F)F 10.1021/jm060662k
CHEMBL219181 90110 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 397 4 1 3 3.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1C(F)(F)F 10.1021/jm060662k
11473427 148285 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL384529 148285 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 5 1 5 3.1 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
11849184 86807 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 364 5 0 5 3.2 CCO/N=C1/c2ccccc2CCC1CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL212901 86807 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 364 5 0 5 3.2 CCO/N=C1/c2ccccc2CCC1CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
11849729 148680 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 362 7 0 5 3.5 CCO/N=C(\CCN1CCN(c2ccccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL386867 148680 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 362 7 0 5 3.5 CCO/N=C(\CCN1CCN(c2ccccc2C#N)CC1)c1ccccc1 10.1021/jm060279f
11325334 86826 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212969 86826 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
2 10035 23 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
54562 10035 23 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
CHEMBL240773 10035 23 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS bindingActivity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060166w
2 10035 23 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
54562 10035 23 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
CHEMBL240773 10035 23 None -2 6 Human 7.3 pEC50 = 7.3 Functional
Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptorEffective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
3038495 7495 37 None -16 6 Human 7.3 pEC50 = 7.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
7625 7495 37 None -16 6 Human 7.3 pEC50 = 7.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
CHEMBL25236 7495 37 None -16 6 Human 7.3 pEC50 = 7.3 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
11849688 86712 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 316 5 1 6 2.5 O/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212545 86712 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 316 5 1 6 2.5 O/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
2 10035 23 None -2 6 Human 8.3 pEC50 = 8.3 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0604979
54562 10035 23 None -2 6 Human 8.3 pEC50 = 8.3 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0604979
CHEMBL240773 10035 23 None -2 6 Human 8.3 pEC50 = 8.3 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0604979
9975465 194430 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL49502 194430 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
228 7233 28 None 1 19 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 7233 28 None 1 19 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 7233 28 None 1 19 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 7233 28 None 1 19 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 7233 28 None 1 19 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
44301054 202927 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL56118 202927 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
11983282 145721 0 None -2 3 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 145721 0 None -2 3 Human 8.3 pEC50 = 8.3 Functional
Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
10088811 90112 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.3 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
CHEMBL219186 90112 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.3 Cc1cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)ccc1F 10.1021/jm060662k
168285556 199696 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 199696 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 199696 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assayAgonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
10064956 143164 5 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3cccc(F)c3)CC2)c1 10.1021/jm060662k
CHEMBL373516 143164 5 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 326 4 1 2 4.0 Cc1cccc(NC(=O)CN2CCC(c3cccc(F)c3)CC2)c1 10.1021/jm060662k
10020098 90115 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cc(C)cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219210 90115 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.8 Cc1cc(C)cc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
10335627 90162 3 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 311 4 1 3 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccc1 10.1021/jm060662k
CHEMBL219426 90162 3 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 311 4 1 3 1.9 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccccc1 10.1021/jm060662k
11849298 86509 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N/O)c1cccc(C)c1 10.1021/jm060279f
CHEMBL211623 86509 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 354 6 1 6 2.4 COC(CN1CCN(c2ccccn2)CC1)/C(=N/O)c1cccc(C)c1 10.1021/jm060279f
155513053 176477 0 None 23 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 176477 0 None 23 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
16094697 144006 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 3 1 3 2.6 [O-][n+]1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm060662k
CHEMBL375120 144006 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 308 3 1 3 2.6 [O-][n+]1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm060662k
11200205 145689 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
CHEMBL378324 145689 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
16094679 90052 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 369 6 1 4 2.9 CC(C)Oc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL218851 90052 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 369 6 1 4 2.9 CC(C)Oc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11314352 86635 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212236 86635 1 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
109030515 182764 1 None 14 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 182764 1 None 14 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
16094677 90111 0 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219185 90111 0 None -1 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11849774 86645 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
CHEMBL212290 86645 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccccc1Cl 10.1021/jm060279f
11849269 86327 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL211415 86327 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(/CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
71452737 85866 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(\CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL2113243 85866 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(\CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
44300865 208774 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL60815 208774 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
16094681 90122 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219261 90122 0 None 1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
44418747 90153 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 3.9 Cc1cccc(Cl)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
CHEMBL219394 90153 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 343 4 1 3 3.9 Cc1cccc(Cl)c1NC(=O)CN1CCC(c2ccccn2)CC1 10.1021/jm060662k
5311189 211620 11 None -2 4 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
CHEMBL7549 211620 11 None -2 4 Human 7.2 pEC50 = 7.2 Functional
Effective concentration required for agonistic activity against human D4.2 receptorEffective concentration required for agonistic activity against human D4.2 receptor
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
11336814 86876 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL213164 86876 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
71456253 85867 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(/CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL2113244 85867 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 399 8 0 5 4.2 CO/N=C(/CCN1CCN(c2ccccc2OC(C)C)CC1)c1ccc(F)cc1 10.1021/jm060279f
11739823 86546 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCCC(c2ccccn2)C1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL211831 86546 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCCC(c2ccccn2)C1)c1ccc(Cl)cc1 10.1021/jm060279f
11151920 86809 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212903 86809 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
109030343 177639 1 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 177639 1 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11849735 145010 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 339 7 0 6 2.4 CCO/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377023 145010 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 339 7 0 6 2.4 CCO/N=C(\CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
10066168 168628 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 345 4 1 3 2.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1 10.1021/jm060662k
CHEMBL414706 168628 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 345 4 1 3 2.8 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(Cl)c1 10.1021/jm060662k
10428816 90123 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 363 4 1 3 2.7 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(F)c(Cl)c1 10.1021/jm060662k
CHEMBL219263 90123 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 363 4 1 3 2.7 O=C(NCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(F)c(Cl)c1 10.1021/jm060662k
11256583 175565 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
CHEMBL437493 175565 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 349 6 0 6 2.5 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
10024158 90116 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 403 4 1 3 3.2 Cc1cc(Br)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219211 90116 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 403 4 1 3 3.2 Cc1cc(Br)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
10404821 175459 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 2.5 C=Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL436527 175459 4 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 337 5 1 3 2.5 C=Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
10383571 90033 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.2 COc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1C 10.1021/jm060662k
CHEMBL218757 90033 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 355 5 1 4 2.2 COc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1C 10.1021/jm060662k
11849687 86781 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(/CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212804 86781 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 311 5 1 6 1.9 O/N=C(/CCN1CCN(c2ncccn2)CC1)c1ccccc1 10.1021/jm060279f
11724450 130626 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 130626 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 130626 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
44400626 77177 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 77177 0 None -2 2 Human 8.1 pEC50 = 8.1 Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
ChEMBL None None None None 10.1021/jm050170s
16094670 90230 5 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cc3)CC2)c1 10.1021/jm060662k
CHEMBL219966 90230 5 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(O)cc3)CC2)c1 10.1021/jm060662k
11772112 175595 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
CHEMBL437687 175595 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
11849779 86670 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
CHEMBL212393 86670 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(C)cc(C)c1 10.1021/jm060279f
16094707 103501 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(C(F)(F)F)c1 10.1021/jm060662k
CHEMBL264286 103501 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 379 4 1 3 3.2 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1cccc(C(F)(F)F)c1 10.1021/jm060662k
16094667 88617 5 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 333 4 1 3 3.7 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C#N)CC2)c1 10.1021/jm060662k
CHEMBL216450 88617 5 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 333 4 1 3 3.7 Cc1cccc(NC(=O)CN2CCC(c3ccccc3C#N)CC2)c1 10.1021/jm060662k
16094700 176502 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3cccc(O)c3)CC2)c1 10.1021/jm060662k
CHEMBL443838 176502 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 324 4 2 3 3.5 Cc1cccc(NC(=O)CN2CCC(c3cccc(O)c3)CC2)c1 10.1021/jm060662k
3645619 9808 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060279f
975 9808 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060279f
CHEMBL45244 9808 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060279f
3645619 9808 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060662k
975 9808 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060662k
CHEMBL45244 9808 20 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm060662k
10737474 108130 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
CHEMBL296953 108130 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
10473658 193972 3 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
CHEMBL49231 193972 3 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligandAgonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
168285560 199697 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 199697 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 199697 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assayPartial agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
155515982 176789 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 176789 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assayAgonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
11849682 87094 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1F 10.1021/jm060279f
CHEMBL214190 87094 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 346 5 1 5 2.8 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1F 10.1021/jm060279f
11849736 145193 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377388 145193 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
11774041 86795 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
CHEMBL212872 86795 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 402 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Br)cc1 10.1021/jm060279f
11394708 86857 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(\CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL213097 86857 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 373 6 0 4 3.6 CO/N=C(\CCN1CCC(c2cccc[n+]2[O-])CC1)c1ccc(Cl)cc1 10.1021/jm060279f
10359645 148314 4 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 336 4 1 4 1.8 N#Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL384690 148314 4 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 336 4 1 4 1.8 N#Cc1cccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
10385883 88346 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C(F)(F)F 10.1021/jm060662k
CHEMBL216215 88346 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 393 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)cc1C(F)(F)F 10.1021/jm060662k
10314506 175455 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1 10.1021/jm060662k
CHEMBL436491 175455 1 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 329 4 1 3 2.3 O=C(CN1CCC(c2cccc[n+]2[O-])CC1)Nc1ccc(F)cc1 10.1021/jm060662k
11772767 86777 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL212784 86777 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
16094676 7020 19 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
8439 7020 19 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
CHEMBL219182 7020 19 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
16094699 88920 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
CHEMBL216794 88920 4 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
9859861 174859 1 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL432579 174859 1 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assayAgonistic activity against human Dopamine receptor D4.2 using [35S]GTP-gamma-S binding assay
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
10314824 42154 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL143761 42154 1 None - 1 Human 8.0 pEC50 = 8.0 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
11849818 84692 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL209447 84692 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 342 6 1 5 3.0 O/N=C(\CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
11983282 145721 0 None -2 3 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 145721 0 None -2 3 Human 8.0 pEC50 = 8.0 Functional
Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assayIntrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
16094665 90244 5 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.0 Cc1cccc(C(=O)NCN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
CHEMBL220083 90244 5 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 315 4 1 4 3.0 Cc1cccc(C(=O)NCN2CCC(c3nccs3)CC2)c1 10.1021/jm060662k
10449865 90045 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1cc(C)cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL218798 90045 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 4 1 3 2.5 Cc1cc(C)cc(C(=O)NCN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
11416883 87905 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
CHEMBL215678 87905 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 352 6 0 5 3.3 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
16094676 7020 19 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
8439 7020 19 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
CHEMBL219182 7020 19 None -1 2 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
15981509 148736 1 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
CHEMBL387250 148736 1 None -3 2 Human 7.0 pEC50 = 7.0 Functional
Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionActivity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
11222637 86558 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
CHEMBL211902 86558 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 376 6 0 5 3.4 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
16094680 90150 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 3 2.7 CCc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219389 90150 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPRAgonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR
ChEMBL 339 5 1 3 2.7 CCc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
44393797 73134 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 412 4 1 4 3.4 Cc1cc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
CHEMBL185149 73134 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5Agonist activity was calculated in calcium flux assay using HEK293 cells co-transfected with human Dopamine receptor D4.4 and Galphaqo5
ChEMBL 412 4 1 4 3.4 Cc1cc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
11849266 87844 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
CHEMBL215450 87844 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
11849781 87096 0 None - 1 Human 7.0 pEC50 = 7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(/CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL214197 87096 0 None - 1 Human 7.0 pEC50 = 7 Functional
Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assayActivity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay
ChEMBL 372 6 0 5 3.7 CO/N=C(/CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
9995904 37993 4 None - 0 Human 8.8 pED50 = 8.8 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140099 37993 4 None - 0 Human 8.8 pED50 = 8.8 Functional
Effective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptorEffective dose was measured by the stimulation of mitogenesis at dopamine D4.2 receptor
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
71458071 86275 0 None - 0 Human 8.1 pED50 = 8.1 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
CHEMBL2113718 86275 0 None - 0 Human 8.1 pED50 = 8.1 Functional
Effective concentration of compound required against human Dopamine D4.2 receptorEffective concentration of compound required against human Dopamine D4.2 receptor
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
9926143 120303 1 None - 1 Human 8.9 pIC50 = 8.9 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL332154 120303 1 None - 1 Human 8.9 pIC50 = 8.9 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
168285556 199696 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 199696 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 199696 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
168277064 199617 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 199617 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 199617 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
168268756 199543 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 199543 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 199543 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
168268756 199543 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 199543 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 199543 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
45361874 176800 2 None 58 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 176800 2 None 58 3 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3303 9024 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 9024 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 9024 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
10021193 73137 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptorInhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptor
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL185156 73137 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptorInhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptor
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
3303 9024 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 9024 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 9024 46 None 1 5 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
109030343 177639 1 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 177639 1 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
135398737 7745 93 None -28 43 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
38 7745 93 None -28 43 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
722 7745 93 None -28 43 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
CHEMBL42 7745 93 None -28 43 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
DB00363 7745 93 None -28 43 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D4 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
155513053 176477 0 None 23 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 176477 0 None 23 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3303 9024 46 None 1 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 9024 46 None 1 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 9024 46 None 1 5 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
16094666 88502 3 None 251 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 88502 3 None 251 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
109030515 182764 1 None 14 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 182764 1 None 14 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168285556 199696 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 199696 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 199696 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
155536720 178966 0 None 37 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 178966 0 None 37 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
168277064 199617 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 199617 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 199617 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
155536815 178986 0 None 13 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
CHEMBL4473792 178986 0 None 13 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
168268756 199543 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 199543 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 199543 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
168285556 199696 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 199696 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 199696 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
168277064 199617 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 199617 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 199617 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
155568411 182859 0 None 2 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4591118 182859 0 None 2 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
155562395 182727 0 None 169 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 182727 0 None 169 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
6466372 176841 12 None 58 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 176841 12 None 58 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
155563301 182029 0 None 10 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 182029 0 None 10 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
9907332 23168 1 None - 1 Human 8.3 pIC50 = 8.3 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
CHEMBL123031 23168 1 None - 1 Human 8.3 pIC50 = 8.3 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
155530763 178348 0 None -2 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 178348 0 None -2 3 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168285560 199697 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 199697 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 199697 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assayAntagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
10425450 6989 30 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 6989 30 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 6989 30 None 125 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
155511803 176384 0 None 1 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4436479 176384 0 None 1 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
155516494 176900 0 None 6 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443848 176900 0 None 6 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
4797946 177203 7 None 81 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 177203 7 None 81 3 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
155568867 182933 0 None -3 3 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 182933 0 None -3 3 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
9948546 23096 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
CHEMBL122754 23096 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2Compound was tested for the inhibition of [3H]thymidine uptake in CHO p-5 cells transfected with human Dopamine receptor D4.2
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
24815434 206475 0 None - 2 Human 7.0 pKi = 7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 305 3 0 3 4.0 Cn1c(CN2CCC(c3ccccc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593196 206475 0 None - 2 Human 7.0 pKi = 7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 305 3 0 3 4.0 Cn1c(CN2CCC(c3ccccc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46225337 206756 0 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 375 3 0 5 3.3 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cn3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595151 206756 0 None - 1 Human 6.0 pKi = 6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 375 3 0 5 3.3 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cn3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
24815976 206538 0 None - 2 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593745 206538 0 None - 2 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
798232 206914 9 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 340 3 0 4 3.5 Cn1c(CN2CCN(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL596271 206914 9 None - 1 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 340 3 0 4 3.5 Cn1c(CN2CCN(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
10615684 24813 0 None 9 2 Human 7.9 pKi = 7.9 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL1202208 24813 0 None 9 2 Human 7.9 pKi = 7.9 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL126493 24813 0 None 9 2 Human 7.9 pKi = 7.9 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
44517726 202801 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
CHEMBL560177 202801 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.06.043
46225583 206953 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nsc4ccccc34)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL596527 206953 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nsc4ccccc34)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
1353 8692 93 None -3 39 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
3559 8692 93 None -3 39 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
86 8692 93 None -3 39 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
CHEMBL54 8692 93 None -3 39 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
DB00502 8692 93 None -3 39 Human 8.7 pKi = 8.7 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
9820304 108846 0 None 10 2 Human 7.6 pKi = 7.6 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL1204116 108846 0 None 10 2 Human 7.6 pKi = 7.6 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL302075 108846 0 None 10 2 Human 7.6 pKi = 7.6 Functional
Antagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cellsAntagonism of dopamine-stimulated [35S]GTP-gamma-S binding against human Dopamine receptor D4 in CHO cells
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
46225334 206825 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 358 3 0 4 3.7 Cn1c(CN2CCN(c3ccc(Cl)cc3F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595607 206825 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 358 3 0 4 3.7 Cn1c(CN2CCN(c3ccc(Cl)cc3F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
24815883 208241 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3cccc(C(F)(F)F)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL604993 208241 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 373 3 0 3 5.0 Cn1c(CN2CCC(c3cccc(C(F)(F)F)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46225581 208766 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3cccc(Cl)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL608103 208766 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3cccc(Cl)c3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46190878 8653 7 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 342 3 0 6 2.3 Clc1cnc(nc1)N1CCN(CC1)Cc1nc2c(n1C)cccc2 10.1016/j.bmcl.2009.11.032
6253 8653 7 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 342 3 0 6 2.3 Clc1cnc(nc1)N1CCN(CC1)Cc1nc2c(n1C)cccc2 10.1016/j.bmcl.2009.11.032
CHEMBL595759 8653 7 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 342 3 0 6 2.3 Clc1cnc(nc1)N1CCN(CC1)Cc1nc2c(n1C)cccc2 10.1016/j.bmcl.2009.11.032
46225584 206454 0 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 408 3 0 4 5.0 Cn1c(CN2CCC(c3ncc(C(F)(F)F)cc3Cl)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593056 206454 0 None - 1 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 408 3 0 4 5.0 Cn1c(CN2CCC(c3ncc(C(F)(F)F)cc3Cl)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
10157556 127013 0 None - 0 Human 8.5 pKi = 8.5 Functional
D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
CHEMBL352207 127013 0 None - 0 Human 8.5 pKi = 8.5 Functional
D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.D4 receptor functional activity was measured inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
3691783 11536 1 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1016/j.bmc.2010.01.040
CHEMBL103871 11536 1 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at dopamine D4 receptorAntagonist activity at dopamine D4 receptor
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1016/j.bmc.2010.01.040
46225335 206826 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595608 206826 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccc(C(F)(F)F)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
24849462 206537 0 None - 1 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL593744 206537 0 None - 1 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 339 3 0 3 4.6 Cn1c(CN2CCC(c3ccc(Cl)cc3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46190877 8652 7 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
6252 8652 7 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
CHEMBL605836 8652 7 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 409 3 0 5 4.0 Clc1cc(cnc1N1CCN(CC1)Cc1nc2c(n1C)cccc2)C(F)(F)F 10.1016/j.bmcl.2009.11.032
46225320 207962 0 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccccc3C(F)(F)F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL603443 207962 0 None - 1 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 374 3 0 4 3.9 Cn1c(CN2CCN(c3ccccc3C(F)(F)F)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
9799123 12391 0 None 61 2 Human 8.2 pKi = 8.2 Functional
Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL107742 12391 0 None 61 2 Human 8.2 pKi = 8.2 Functional
Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine D4 receptor functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
46225582 208394 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL605831 208394 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 362 3 0 5 4.6 Cn1c(CN2CCC(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
46225336 206827 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 363 3 0 6 3.5 Cn1c(CN2CCN(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
CHEMBL595609 206827 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assayAntagonist activity at human D4 receptor expressed in HEK293 cells co-expressing Gqo5 G-protein by FLIPR assay
ChEMBL 363 3 0 6 3.5 Cn1c(CN2CCN(c3nc4ccccc4s3)CC2)nc2ccccc21 10.1016/j.bmcl.2009.11.032
9952003 12132 0 None - 0 Human 6.0 pKi = 6.0 Functional
Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106916 12132 0 None - 0 Human 6.0 pKi = 6.0 Functional
Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.Dopamine Receptor D4 functional activity was assessed via inhibition of quinpirole stimulated [35S]GTP-gamma-S binding from cell membranes.
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
681 8247 72 None -1 14 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 None -1 14 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 None -1 14 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 None -1 14 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 None -1 14 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
228 7233 28 None 1 19 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 7233 28 None 1 19 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 7233 28 None 1 19 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 7233 28 None 1 19 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 7233 28 None 1 19 Rat 8.1 pEC50 = 8.1 Functional
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
30699 224483 0 None -1 14 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 423 7 2 8 0.5 CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O None
4223 10764 94 None -588 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 10764 94 None -588 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 10764 94 None -588 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 10764 94 None -588 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 10764 94 None -588 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
10263487 9843 0 None -19 2 Human 5.4 pIC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 4 1.8 CCCN1C[C@H](OC[C@@H]1C)c1ccc(nc1)N 22470105
7683 9843 0 None -19 2 Human 5.4 pIC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 235 3 1 4 1.8 CCCN1C[C@H](OC[C@@H]1C)c1ccc(nc1)N 22470105


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

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 DOI
124087 8171 114 None - 15 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 8171 114 None - 15 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 8171 114 None - 15 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 8171 114 None - 15 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 8171 114 None - 15 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
5329102 201505 86 None - 0 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 201505 86 None - 0 Human 7.0 pAC50 = 7.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
1353 8692 93 None -3 85 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 8692 93 None -3 85 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 8692 93 None -3 85 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 8692 93 None -3 85 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 8692 93 None -3 85 Human 7.9 pAC50 = 7.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
1782 9296 84 None - 23 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
241 9296 84 None - 23 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
4168 9296 84 None - 23 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
CHEMBL86 9296 84 None - 23 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
DB01233 9296 84 None - 23 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC 10.1038/s41467-023-40064-9
213 10625 55 None -6 43 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 10625 55 None -6 43 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 10625 55 None -6 43 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 10625 55 None -6 43 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 10625 55 None -6 43 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2247 7293 81 None -63 42 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 7293 81 None -63 42 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 7293 81 None -63 42 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 7293 81 None -63 42 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 7293 81 None -63 42 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
1613 9127 53 None -2 44 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 9127 53 None -2 44 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 9127 53 None -2 44 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 9127 53 None -2 44 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 9127 53 None -2 44 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2337 10030 77 None -114 62 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 10030 77 None -114 62 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 10030 77 None -114 62 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 10030 77 None -114 62 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 10030 77 None -114 62 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
2585 7590 103 None - 22 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 7590 103 None - 22 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 7590 103 None - 22 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 7590 103 None - 22 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 7590 103 None - 22 Human 7.8 pAC50 = 7.8 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
3294 8787 111 None -11 44 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 8787 111 None -11 44 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 8787 111 None -11 44 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 8787 111 None -11 44 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 8787 111 None -11 44 Human 7.7 pAC50 = 7.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
3883 190314 112 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
CHEMBL480 190314 112 None - 0 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 369 5 1 4 3.5 Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1 10.1038/s41467-023-40064-9
135 9310 43 None - 56 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 9310 43 None - 56 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 9310 43 None - 56 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 9310 43 None - 56 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 9310 43 None - 56 Human 5.7 pAC50 = 5.7 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
2865 10915 73 None -66 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 10915 73 None -66 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 10915 73 None -66 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 10915 73 None -66 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 10915 73 None -66 53 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
36811 8236 37 None - 7 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
535 8236 37 None - 7 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
937 8236 37 None - 7 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL926 8236 37 None - 7 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00841 8236 37 None - 7 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
1890 9535 49 None - 16 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 9535 49 None - 16 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 9535 49 None - 16 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 9535 49 None - 16 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 9535 49 None - 16 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
2286 9957 51 None - 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 9957 51 None - 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 9957 51 None - 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 9957 51 None - 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 9957 51 None - 30 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
2389 10104 118 None -22 66 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 10104 118 None -22 66 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 10104 118 None -22 66 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 10104 118 None -22 66 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 10104 118 None -22 66 Human 8.4 pAC50 = 8.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
3180 21245 41 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201217 21245 41 None - 0 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 289 8 0 3 3.9 CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1 10.1038/s41467-023-40064-9
5411 210812 89 None - 2 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL698 210812 89 None - 2 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 264 8 1 4 2.6 CCCCNc1ccc(C(=O)OCCN(C)C)cc1 10.1038/s41467-023-40064-9
135398737 7745 93 None -13 90 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 7745 93 None -13 90 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 7745 93 None -13 90 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 7745 93 None -13 90 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 7745 93 None -13 90 Human 7.4 pAC50 = 7.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
4034 62596 55 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 62596 55 None - 1 Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
242 7258 124 None -104 51 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 7258 124 None -104 51 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 7258 124 None -104 51 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 7258 124 None -104 51 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 7258 124 None -104 51 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
191 7191 98 None -8 29 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 7191 98 None -8 29 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 7191 98 None -8 29 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 7191 98 None -8 29 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 7191 98 None -8 29 Human 7.3 pAC50 = 7.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
10831 123741 25 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL338667 123741 25 None - 0 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 397 7 2 5 4.3 O=C(Nc1ccccc1)OCC(CN1CCCCC1)OC(=O)Nc1ccccc1 10.1038/s41467-023-40064-9
2284 9956 33 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 9956 33 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 9956 33 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 9956 33 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 9956 33 None - 29 Human 6.3 pAC50 = 6.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
1427 8794 54 None - 27 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 8794 54 None - 27 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 8794 54 None - 27 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 8794 54 None - 27 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 8794 54 None - 27 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
135398745 9688 112 None -10 65 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 9688 112 None -10 65 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 9688 112 None -10 65 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 9688 112 None -10 65 Human 7.2 pAC50 = 7.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
5472 212597 75 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL1717 212597 75 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
CHEMBL833 212597 75 None - 3 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 263 2 0 2 4.0 Clc1ccccc1CN1CCc2sccc2C1 10.1038/s41467-023-40064-9
135409453 10545 41 None - 2 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 10545 41 None - 2 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 10545 41 None - 2 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
16362 9899 71 None -20 29 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 9899 71 None -20 29 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 9899 71 None -20 29 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 9899 71 None -20 29 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 9899 71 None -20 29 Human 7.1 pAC50 = 7.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3158 63041 27 None - 20 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 63041 27 None - 20 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
212 10578 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 10578 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 10578 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 10578 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 10578 47 None -6 25 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
180 7189 56 None - 40 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 7189 56 None - 40 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 7189 56 None - 40 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 7189 56 None - 40 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 7189 56 None - 40 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3152 195190 103 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
CHEMBL502 195190 103 None - 0 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
1400 8738 70 None - 3 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 8738 70 None - 3 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 8738 70 None - 3 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 8738 70 None - 3 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 8738 70 None - 3 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 8738 70 None - 3 Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
21722 24764 31 None - 6 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 24764 31 None - 6 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD4 in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
14925759 164817 6 None 18 13 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 164817 6 None 18 13 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL5290993 201298 0 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 301 2 1 2 3.0 CC(C)N1C[C@H](NC(=O)N2Cc3ccccc3[C@@H]2C)[C@@H](C)C1 10.1016/j.ejmech.2020.113141
9945233 211871 1 None - 1 Human 9.0 pEC50 = 9 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL77563 211871 1 None - 1 Human 9.0 pEC50 = 9 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
25131876 92967 0 None -12 7 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2020.113141
CHEMBL2312227 92967 0 None -12 7 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2020.113141
228 7233 28 None - 23 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 7233 28 None - 23 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 7233 28 None - 23 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 7233 28 None - 23 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 7233 28 None - 23 Rat 8.8 pEC50 = 8.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL5277789 200727 0 None -7 2 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 405 8 2 5 3.7 Oc1cccc(OCCNCC2COCC(c3ccccc3)(c3ccccc3)O2)c1 10.1016/j.ejmech.2020.113141
CHEMBL5272829 200516 0 None - 1 Human 8.0 pEC50 = 8 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 320 6 1 3 3.8 CCS[C@H]1CC[C@@H](N(C)CC(=O)Nc2ccc(C)c(C)c2)C1 10.1016/j.ejmech.2020.113141
9857248 211883 6 None - 1 Human 8.0 pEC50 = 8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77708 211883 6 None - 1 Human 8.0 pEC50 = 8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
10268039 24788 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 321 4 1 3 4.0 COc1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL126361 24788 0 None - 0 Human 7.0 pEC50 = 7 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 321 4 1 3 4.0 COc1ccccc1C1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
44315403 212250 0 None - 1 Human 5.0 pEC50 = 5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
CHEMBL80469 212250 0 None - 1 Human 5.0 pEC50 = 5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
CHEMBL5283608 200999 0 None - 1 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 345 6 0 6 3.0 CCOC(=O)c1nn(-c2ccccc2)cc1CN(C)[C@@H]1CCSC1 10.1016/j.ejmech.2020.113141
164612037 192156 0 None -1 20 Human 7.0 pEC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 192156 0 None -1 20 Human 7.0 pEC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
11392147 24860 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 290 3 1 3 3.2 C1=C(c2ccccn2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
CHEMBL126754 24860 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 290 3 1 3 3.2 C1=C(c2ccccn2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
681 8247 72 None -2 38 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
940 8247 72 None -2 38 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
947 8247 72 None -2 38 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
CHEMBL59 8247 72 None -2 38 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
DB00988 8247 72 None -2 38 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
5025739 175975 45 None 30 2 Human 7.9 pEC50 = 7.9 Binding
D4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cellsD4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
CHEMBL440687 175975 45 None 30 2 Human 7.9 pEC50 = 7.9 Binding
D4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cellsD4 efficacy was measured using recombinant human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
4826074 110881 6 None - 1 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL309372 110881 6 None - 1 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
5025739 175975 45 None 30 2 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL440687 175975 45 None 30 2 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
9836662 104929 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 318 3 1 5 2.2 N#Cc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL273772 104929 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 318 3 1 5 2.2 N#Cc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
45361874 176800 2 None 48 3 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 176800 2 None 48 3 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11474209 124152 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 371 4 1 6 1.7 CS(=O)(=O)c1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL339791 124152 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 371 4 1 6 1.7 CS(=O)(=O)c1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
9835713 25258 1 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL127226 25258 1 None - 0 Human 7.9 pEC50 = 7.9 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 3.3 c1ccc(C2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
5025739 175975 45 None - 2 Rat 7.8 pEC50 = 7.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL440687 175975 45 None - 2 Rat 7.8 pEC50 = 7.8 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
9858141 124407 1 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 317 3 1 4 2.8 N#Cc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL340099 124407 1 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 317 3 1 4 2.8 N#Cc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
9901273 24817 3 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL126510 24817 3 None - 0 Human 7.8 pEC50 = 7.8 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
119570 9933 96 None -6 39 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
2233 9933 96 None -6 39 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
953 9933 96 None -6 39 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
CHEMBL301265 9933 96 None -6 39 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
DB00413 9933 96 None -6 39 Human 7.8 pEC50 = 7.8 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
10336538 8406 50 None -3 8 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
974 8406 50 None -3 8 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
CHEMBL310843 8406 50 None -3 8 Human 6.8 pEC50 = 6.8 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
5281239 57407 48 None - 0 Human 4.8 pEC50 = 4.8 Binding
Agonist activity at D4R (unknown origin)Agonist activity at D4R (unknown origin)
ChEMBL 658 11 2 6 8.7 CC(=O)O[C@H]1CC(C)(C)C(=C=C/C(C)=C/C=C/C(C)=C/C=C/C=C(C)/C=C/C=C(\C)C(=O)C[C@@]23O[C@]2(C)C[C@@H](O)CC3(C)C)[C@](C)(O)C1 10.1016/j.ejmech.2020.113141
CHEMBL1575074 57407 48 None - 0 Human 4.8 pEC50 = 4.8 Binding
Agonist activity at D4R (unknown origin)Agonist activity at D4R (unknown origin)
ChEMBL 658 11 2 6 8.7 CC(=O)O[C@H]1CC(C)(C)C(=C=C/C(C)=C/C=C/C(C)=C/C=C/C=C(C)/C=C/C=C(\C)C(=O)C[C@@]23O[C@]2(C)C[C@@H](O)CC3(C)C)[C@](C)(O)C1 10.1016/j.ejmech.2020.113141
CHEMBL5267339 200299 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 340 5 1 5 3.1 Clc1ccc(-n2cc(CNC[C@@H]3CCCOC3)nn2)c(Cl)c1 10.1016/j.ejmech.2020.113141
681 8247 72 None -2 38 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
940 8247 72 None -2 38 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
947 8247 72 None -2 38 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
CHEMBL59 8247 72 None -2 38 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
DB00988 8247 72 None -2 38 Human 8.7 pEC50 = 8.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
681 8247 72 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
940 8247 72 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
947 8247 72 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
CHEMBL59 8247 72 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
DB00988 8247 72 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
681 8247 72 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
940 8247 72 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
947 8247 72 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
CHEMBL59 8247 72 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
DB00988 8247 72 None -7 38 Rat 8.6 pEC50 = 8.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm030505a
16759175 61768 21 None - 1 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D4RAgonist activity at human D4R
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
CHEMBL1334895 61768 21 None - 1 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D4RAgonist activity at human D4R
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
CHEMBL1616116 61768 21 None - 1 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D4RAgonist activity at human D4R
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
CHEMBL5289845 201261 0 None - 1 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 346 7 3 4 2.7 O=c1cc(CNC[C@@H](CO)Cc2ccsc2)[nH]c2ccc(F)cc12 10.1016/j.ejmech.2020.113141
973 7960 39 None 9 6 Rat 7.7 pEC50 = 7.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 7960 39 None 9 6 Rat 7.7 pEC50 = 7.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 7960 39 None 9 6 Rat 7.7 pEC50 = 7.7 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
3303 9024 46 None 1 15 Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
5311200 9024 46 None 1 15 Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
CHEMBL267014 9024 46 None 1 15 Human 5.7 pEC50 = 5.7 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
168294767 199798 0 None -1 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 199798 0 None -1 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 199798 0 None -1 20 Human 5.7 pEC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
9838927 25592 11 None - 0 Human 6.6 pEC50 = 6.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 289 3 1 2 3.9 C1=C(c2ccccc2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
CHEMBL127930 25592 11 None - 0 Human 6.6 pEC50 = 6.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human D4.4 receptor using FLIPR assay
ChEMBL 289 3 1 2 3.9 C1=C(c2ccccc2)CCN(Cc2nc3ccccc3[nH]2)C1 10.1021/jm030505a
11255258 25605 4 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 4 1 4 2.3 c1ccc(N2CCN(CCc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL128040 25605 4 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 4 1 4 2.3 c1ccc(N2CCN(CCc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
5025739 175975 45 None - 2 Rat 7.6 pEC50 = 7.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL440687 175975 45 None - 2 Rat 7.6 pEC50 = 7.6 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL5278957 200784 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 363 3 2 2 3.4 CC(C)N1C[C@H](C)[C@H](NC(=O)c2cc3ccc(Br)cc3[nH]2)C1 10.1016/j.ejmech.2020.113141
9966489 24848 1 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL126687 24848 1 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1cccnc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
16094666 88502 3 None 52 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 88502 3 None 52 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
9945714 25491 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 336 5 1 4 3.3 CCOc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL127752 25491 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 336 5 1 4 3.3 CCOc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
155515982 176789 0 None 6 17 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 176789 0 None 6 17 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
155568867 182933 0 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 182933 0 None - 1 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
6466372 176841 12 None 93 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 176841 12 None 93 3 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3716121 90856 16 None 70 5 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human D4R assessed as [35S] GTPgammaS bindingAgonist activity at human D4R assessed as [35S] GTPgammaS binding
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.ejmech.2020.113141
CHEMBL2207643 90856 16 None 70 5 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human D4R assessed as [35S] GTPgammaS bindingAgonist activity at human D4R assessed as [35S] GTPgammaS binding
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.ejmech.2020.113141
9945753 23640 4 None - 0 Human 8.4 pEC50 = 8.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 337 4 1 5 2.8 O=[N+]([O-])c1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL124927 23640 4 None - 0 Human 8.4 pEC50 = 8.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 337 4 1 5 2.8 O=[N+]([O-])c1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
9857248 211883 6 None - 1 Human 7.5 pEC50 = 7.5 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm030505a
CHEMBL77708 211883 6 None - 1 Human 7.5 pEC50 = 7.5 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm030505a
CHEMBL5277325 200711 0 None 35 2 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at D4R (unknown origin) assessed as beta-arrestin recruitmentAgonist activity at D4R (unknown origin) assessed as beta-arrestin recruitment
ChEMBL 343 7 2 2 3.5 CN(C)[C@@H](CNC(=O)NC[C@H]1Cc2ccccc21)CC1CCCCC1 10.1016/j.ejmech.2020.113141
973 7960 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm0305669
9796720 7960 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm0305669
CHEMBL77395 7960 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm0305669
973 7960 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 7960 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 7960 39 None -9 6 Human 7.5 pEC50 = 7.5 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
155559617 181663 0 None 9 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 181663 0 None 9 3 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
137646281 164585 0 None -1659 17 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 164585 0 None -1659 17 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
973 7960 39 None 9 6 Rat 7.4 pEC50 = 7.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 7960 39 None 9 6 Rat 7.4 pEC50 = 7.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 7960 39 None 9 6 Rat 7.4 pEC50 = 7.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9879627 23828 1 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.6 Cc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)n1 10.1021/jm030505a
CHEMBL125464 23828 1 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.6 Cc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)n1 10.1021/jm030505a
4797946 177203 7 None 165 3 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 177203 7 None 165 3 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
72901200 126555 25 None 154 4 Human 8.4 pEC50 = 8.4 Binding
Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5210121
CHEMBL3480577 126555 25 None 154 4 Human 8.4 pEC50 = 8.4 Binding
Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4Affinity On-target Cellular interaction (Split luciferase based cAMP receptor assay (HEK293T cells)) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5210121
72901200 126555 25 None 154 4 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.1016/j.ejmech.2020.113141
CHEMBL3480577 126555 25 None 154 4 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.1016/j.ejmech.2020.113141
228 7233 28 None -1 23 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 7233 28 None -1 23 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 7233 28 None -1 23 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 7233 28 None -1 23 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 7233 28 None -1 23 Human 8.4 pEC50 = 8.4 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
10225902 24850 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 449 3 1 4 3.8 Brc1cc(Br)c2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
CHEMBL126698 24850 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 449 3 1 4 3.8 Brc1cc(Br)c2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
10014924 114048 0 None -16 5 Human 5.4 pEC50 = 5.4 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
CHEMBL316983 114048 0 None -16 5 Human 5.4 pEC50 = 5.4 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
9922161 24830 6 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
CHEMBL126595 24830 6 None - 0 Human 7.4 pEC50 = 7.4 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm030505a
10425450 6989 30 None -1 4 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 6989 30 None -1 4 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 6989 30 None -1 4 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
228 7233 28 None - 23 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
33 7233 28 None - 23 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
6005 7233 28 None - 23 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
CHEMBL53 7233 28 None - 23 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
DB00714 7233 28 None - 23 Rat 8.3 pEC50 = 8.3 Binding
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assayIn vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm030505a
4826074 110881 6 None - 1 Human 8.3 pEC50 = 8.3 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL309372 110881 6 None - 1 Human 8.3 pEC50 = 8.3 Binding
Effective concentration against human Dopamine receptor D4Effective concentration against human Dopamine receptor D4
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
44381216 127110 0 None 8511 4 Human 7.3 pEC50 = 7.3 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL352925 127110 0 None 8511 4 Human 7.3 pEC50 = 7.3 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
155552185 180840 0 None 2 16 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 180840 0 None 2 16 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
9815072 24822 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
CHEMBL126530 24822 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
CHEMBL5290570 201282 0 None - 1 Human 5.2 pEC50 = 5.2 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 334 4 1 6 2.1 CCOC(=O)c1sc2[nH]cn/c(=N\[C@H]3CCN(CC)C3)c2c1C 10.1016/j.ejmech.2020.113141
3645619 9808 20 None -5 9 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
975 9808 20 None -5 9 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
CHEMBL45244 9808 20 None -5 9 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
9836209 24821 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
CHEMBL126529 24821 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 307 3 1 4 2.7 C[C@@H]1CN(c2ccccn2)CCN1Cc1nc2ccccc2[nH]1 10.1021/jm030505a
168290235 199747 0 None -5 20 Human 5.2 pEC50 = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 199747 0 None -5 20 Human 5.2 pEC50 = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 199747 0 None -5 20 Human 5.2 pEC50 = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168295528 199810 0 None -1 20 Human 6.2 pEC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 199810 0 None -1 20 Human 6.2 pEC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 199810 0 None -1 20 Human 6.2 pEC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
9945233 211871 1 None - 1 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL77563 211871 1 None - 1 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
11724450 130626 4 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL184158 130626 4 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL362542 130626 4 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human D4R expressed in HEK293 cells by calcium flux assayAgonist activity at human D4R expressed in HEK293 cells by calcium flux assay
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
9857887 25301 2 None - 0 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1ccc2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
CHEMBL127460 25301 2 None - 0 Human 8.1 pEC50 = 8.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 311 3 1 4 2.4 Fc1ccc2[nH]c(CN3CCN(c4ccccn4)CC3)nc2c1 10.1021/jm030505a
2 10035 23 None -2 28 Human 8.1 pEC50 = 8.1 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
54562 10035 23 None -2 28 Human 8.1 pEC50 = 8.1 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
CHEMBL240773 10035 23 None -2 28 Human 8.1 pEC50 = 8.1 Binding
Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
5281239 57407 48 None - 0 Human 4.1 pEC50 = 4.1 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 658 11 2 6 8.7 CC(=O)O[C@H]1CC(C)(C)C(=C=C/C(C)=C/C=C/C(C)=C/C=C/C=C(C)/C=C/C=C(\C)C(=O)C[C@@]23O[C@]2(C)C[C@@H](O)CC3(C)C)[C@](C)(O)C1 10.1016/j.ejmech.2020.113141
CHEMBL1575074 57407 48 None - 0 Human 4.1 pEC50 = 4.1 Binding
Agonist activity at D4R (unknown origin) by camp reporter assayAgonist activity at D4R (unknown origin) by camp reporter assay
ChEMBL 658 11 2 6 8.7 CC(=O)O[C@H]1CC(C)(C)C(=C=C/C(C)=C/C=C/C(C)=C/C=C/C=C(C)/C=C/C=C(\C)C(=O)C[C@@]23O[C@]2(C)C[C@@H](O)CC3(C)C)[C@](C)(O)C1 10.1016/j.ejmech.2020.113141
2 10035 23 None -2 28 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
54562 10035 23 None -2 28 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
CHEMBL240773 10035 23 None -2 28 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assayAgonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01085
9881000 123717 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 338 4 1 4 3.6 CSc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
CHEMBL338547 123717 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
In vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assayIn vitro EC50 tested on HEK293 cells co-transfected with human Dopamine receptor D4.4 using FLIPR assay
ChEMBL 338 4 1 4 3.6 CSc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm030505a
1588 9105 27 None -16 44 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.9b00412
28864 9105 27 None -16 44 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.9b00412
43 9105 27 None -16 44 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.9b00412
CHEMBL157138 9105 27 None -16 44 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.9b00412
DB00589 9105 27 None -16 44 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/acs.jmedchem.9b00412
2 10035 23 None -2 28 Human 8.0 pEC50 = 8 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
54562 10035 23 None -2 28 Human 8.0 pEC50 = 8 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
CHEMBL240773 10035 23 None -2 28 Human 8.0 pEC50 = 8 Binding
Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptorEffective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
681 8247 72 None -2 38 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
940 8247 72 None -2 38 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
947 8247 72 None -2 38 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
CHEMBL59 8247 72 None -2 38 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
DB00988 8247 72 None -2 38 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assayAgonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b00265
155536720 178966 0 None 77 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 178966 0 None 77 3 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
3626837 214094 11 None 125 4 Human 10.2 pIC50 = 10.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
CHEMBL93403 214094 11 None 125 4 Human 10.2 pIC50 = 10.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
2470 10425 50 None -20 58 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
3300 10425 50 None -20 58 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
5265 10425 50 None -20 58 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
99 10425 50 None -20 58 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
CHEMBL267930 10425 50 None -20 58 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
14925759 164817 6 None 18 13 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 164817 6 None 18 13 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
3303 9024 46 None 1 15 Human 9.0 pIC50 = 9 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
5311200 9024 46 None 1 15 Human 9.0 pIC50 = 9 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
CHEMBL267014 9024 46 None 1 15 Human 9.0 pIC50 = 9 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
10783358 46441 4 None 42 2 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm981041x
CHEMBL147483 46441 4 None 42 2 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm981041x
10406796 106778 10 None -19 4 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL286725 106778 10 None -19 4 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
11738728 25271 0 None - 1 Human 9.0 pIC50 = 9 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
CHEMBL127290 25271 0 None - 1 Human 9.0 pIC50 = 9 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
1353 8692 93 None -3 85 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
3559 8692 93 None -3 85 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
86 8692 93 None -3 85 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
CHEMBL54 8692 93 None -3 85 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
DB00502 8692 93 None -3 85 Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981041x
9104271 210776 12 None 436 2 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1021/jm058225d
CHEMBL69584 210776 12 None 436 2 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1021/jm058225d
10497674 24779 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL1202219 24779 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL126322 24779 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm990562x
10570563 24802 0 None 15 2 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL1202212 24802 0 None 15 2 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL126429 24802 0 None 15 2 Human 8.0 pIC50 = 8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
127030612 146108 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792725 146108 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
127029391 146126 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792907 146126 0 None - 1 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
118714552 121305 0 None 97 2 Human 7.0 pIC50 = 7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335555 121305 0 None 97 2 Human 7.0 pIC50 = 7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL5288557 201210 0 None - 0 Human 5.0 pIC50 = 5 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 535 9 1 5 5.4 O=C(Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2ccccc21)NCc1ccccc1 10.1021/acs.jmedchem.1c00704
135512187 41373 5 None - 0 Human 5.0 pIC50 = 5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccccc3O)CC2)nc2ccccc12 nan
CHEMBL1429613 41373 5 None - 0 Human 5.0 pIC50 = 5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccccc3O)CC2)nc2ccccc12 nan
168276065 196999 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5174753 196999 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
127030606 146140 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793033 146140 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
155516494 176900 0 None 269 2 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443848 176900 0 None 269 2 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168296347 199241 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208643 199241 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
109030343 177639 1 None 15 3 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 177639 1 None 15 3 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
127028185 146114 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792751 146114 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
16104 168696 19 None -1 5 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm991005d
CHEMBL415300 168696 19 None -1 5 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm991005d
135398737 7745 93 None -13 90 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
38 7745 93 None -13 90 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
722 7745 93 None -13 90 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
CHEMBL42 7745 93 None -13 90 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
DB00363 7745 93 None -13 90 Human 7.0 pIC50 = 7.0 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
10645208 42963 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 7 0 6 4.2 COc1cccc(-c2csc(CCN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL144494 42963 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 7 0 6 4.2 COc1cccc(-c2csc(CCN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL2373205 42963 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 7 0 6 4.2 COc1cccc(-c2csc(CCN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
9868793 103752 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Percent inhibition towards dopamine D4 receptorPercent inhibition towards dopamine D4 receptor
ChEMBL 458 8 1 8 2.8 COc1nsnc1N1CCN(C[C@@H](Cc2cccnc2)NC(=O)C2(C)CCCCC2)CC1 10.1016/s0960-894x(01)00151-2
CHEMBL266393 103752 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Percent inhibition towards dopamine D4 receptorPercent inhibition towards dopamine D4 receptor
ChEMBL 458 8 1 8 2.8 COc1nsnc1N1CCN(C[C@@H](Cc2cccnc2)NC(=O)C2(C)CCCCC2)CC1 10.1016/s0960-894x(01)00151-2
127053218 146256 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794336 146256 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
1016 10519 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 10519 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 10519 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 10519 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 10519 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 10519 78 None -28 35 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
70788951 33928 1 None -1 5 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
CHEMBL1366 33928 1 None -1 5 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
72737750 121301 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335543 121301 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
168288343 198236 0 None 1 2 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5193214 198236 0 None 1 2 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5290330 201275 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 452 5 0 4 3.8 CC(C)(C)N1C=CN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1=O 10.1021/acs.jmedchem.1c00704
10236758 122550 5 None 208 13 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 122550 5 None 208 13 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
242 7258 124 None -104 51 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
34 7258 124 None -104 51 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
60795 7258 124 None -104 51 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
CHEMBL1112 7258 124 None -104 51 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
DB01238 7258 124 None -104 51 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
9954899 211242 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL72292 211242 17 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
44363755 128637 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccccc1N1CCN(CCC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
CHEMBL359002 128637 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccccc1N1CCN(CCC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
135398737 7745 93 None -13 90 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
38 7745 93 None -13 90 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
722 7745 93 None -13 90 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
CHEMBL42 7745 93 None -13 90 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
DB00363 7745 93 None -13 90 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4.4 receptorInhibition of human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2010.07.034
168270809 196827 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5172055 196827 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
118719926 122558 0 None 102 8 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354073 122558 0 None 102 8 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL5275349 200629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 683 8 1 5 7.1 O=C(Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2cc(Br)c(Br)cc21)NC1CCCCC1 10.1021/acs.jmedchem.1c00704
CHEMBL5280677 200855 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 478 6 0 4 4.4 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)N1C=CN(C2CCCCC2)C(=O)C1 10.1021/acs.jmedchem.1c00704
3191 109635 97 None -10 25 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 109635 97 None -10 25 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
127032084 146119 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792813 146119 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127031500 146128 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792931 146128 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127031201 146153 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793131 146153 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
127031830 146210 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793906 146210 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
127031513 146252 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794287 146252 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
72737723 9356 1 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
8440 9356 1 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
CHEMBL3335556 9356 1 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
9904205 212629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL83658 212629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(02)00796-5
9904205 212629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL83658 212629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 294 2 0 3 3.4 CN(C)CC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
10594723 23816 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL125455 23816 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
163322330 197479 3 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5182191 197479 3 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
168287664 198431 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5196102 198431 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
168273063 197064 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5175728 197064 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
16094666 88502 3 None 52 3 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 88502 3 None 52 3 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
2726 7706 68 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 7706 68 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 7706 68 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 7706 68 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 7706 68 None -8 72 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
135398737 7745 93 None -13 90 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
38 7745 93 None -13 90 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
722 7745 93 None -13 90 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
CHEMBL42 7745 93 None -13 90 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
DB00363 7745 93 None -13 90 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058225d
168293190 198909 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5203595 198909 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5274482 200598 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 442 7 1 4 3.3 CN(CC(=O)NC(C)(C)C)C(=O)CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00704
1613 9127 53 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
205 9127 53 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
3964 9127 53 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
CHEMBL831 9127 53 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
DB00408 9127 53 None -2 44 Human 7.9 pIC50 = 7.9 Binding
Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2Compound was tested in vitro for its binding affinity towards human Dopamine receptor D4.2
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm991005d
44318454 212788 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL84931 212788 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 312 2 0 3 3.5 CN(C)CC1CC2c3ccccc3Cc3ccc(F)cc3N2O1 10.1016/s0960-894x(01)00721-1
10894144 117336 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 377 7 0 4 3.5 N#Cc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1 10.1021/jm010878g
CHEMBL325258 117336 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 377 7 0 4 3.5 N#Cc1ccc(CCOC(=O)N2CCN(CCCc3ccccc3)CC2)cc1 10.1021/jm010878g
168277992 196907 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5173368 196907 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
100 10577 58 None -8 54 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 10577 58 None -8 54 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 10577 58 None -8 54 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 10577 58 None -8 54 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 10577 58 None -8 54 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
168269421 196741 0 None 6 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170670 196741 0 None 6 3 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
20354789 121302 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335544 121302 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
10026300 174613 17 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL430798 174613 17 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
93601125 146129 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
CHEMBL3792941 146129 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
127053198 146150 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793112 146150 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127029390 146261 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794421 146261 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
118719926 122558 0 None 102 8 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354073 122558 0 None 102 8 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
168282745 197874 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5187721 197874 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
4189 213701 96 None -33 34 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 213701 96 None -33 34 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 213701 96 None -33 34 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
135398737 7745 93 None -13 90 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
38 7745 93 None -13 90 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
722 7745 93 None -13 90 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
CHEMBL42 7745 93 None -13 90 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
DB00363 7745 93 None -13 90 Human 6.8 pIC50 = 6.8 Binding
Percent inhibition against Dopamine receptor D4 at 1 uMPercent inhibition against Dopamine receptor D4 at 1 uM
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm058018d
168297637 199102 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5206427 199102 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5280979 200870 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 527 8 1 5 5.5 O=C(Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2ccccc21)NC1CCCCC1 10.1021/acs.jmedchem.1c00704
21186194 210014 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL64487 210014 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
10739194 123604 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1c(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL1202204 123604 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1c(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
CHEMBL337951 123604 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1c(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/jm990562x
127053215 146202 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793858 146202 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
72737744 121296 0 None 64 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335538 121296 0 None 64 3 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
168275962 197398 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5180979 197398 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5278239 200749 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 476 9 1 4 3.7 CN(CC(=O)NCc1ccccc1)C(=O)CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00704
10713599 26174 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cc(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL1202225 26174 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cc(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL129324 26174 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cc(Cl)cc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
168275089 197275 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5179198 197275 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
168279825 197595 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5183902 197595 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
168283295 198014 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5189986 198014 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
168291848 198651 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5199552 198651 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
137640201 163740 2 None 177 13 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 163740 2 None 177 13 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
168290895 198778 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5201507 198778 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
168292124 198804 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5201917 198804 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
44342270 16702 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
CHEMBL114484 16702 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
21186143 210057 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL64671 210057 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
135398737 7745 93 None -13 90 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
38 7745 93 None -13 90 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
722 7745 93 None -13 90 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
CHEMBL42 7745 93 None -13 90 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
DB00363 7745 93 None -13 90 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm990562x
9797161 123671 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL1204119 123671 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL338337 123671 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
127032086 146100 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
CHEMBL3792637 146100 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
72737728 121297 0 None 60 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335539 121297 0 None 60 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
135398745 9688 112 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
47 9688 112 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
CHEMBL715 9688 112 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
DB00334 9688 112 None -10 65 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
168292951 198927 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5203807 198927 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
176 7186 66 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -4 31 Human 4.8 pIC50 = 4.8 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
53320010 63438 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642117 63438 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2cccc3c2C(=O)CCN3S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2010.12.007
127031832 146193 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793782 146193 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
127030909 146259 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794375 146259 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
60149678 121295 0 None 229 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335537 121295 0 None 229 2 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
42 8844 57 None - 18 Human 5.8 pIC50 = 5.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm040792y
56971 8844 57 None - 18 Human 5.8 pIC50 = 5.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm040792y
CHEMBL8412 8844 57 None - 18 Human 5.8 pIC50 = 5.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm040792y
168279082 197512 0 None -1 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5182602 197512 0 None -1 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
168280464 197515 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
CHEMBL5182635 197515 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
45109862 14206 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
CHEMBL1086626 14206 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 470 7 2 3 5.2 Cc1[nH]c(-c2ccccc2)cc1C(=O)NCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2010.01.093
168271806 197298 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5179482 197298 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
10981761 117415 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 379 3 1 6 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3nsnc3c1)CC2 10.1021/jm010878g
CHEMBL325750 117415 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 379 3 1 6 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3nsnc3c1)CC2 10.1021/jm010878g
127031831 146118 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792805 146118 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10425450 6989 30 None -1 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 6989 30 None -1 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 6989 30 None -1 4 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
168280776 197937 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5188602 197937 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
6466372 176841 12 None 93 3 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 176841 12 None 93 3 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168275381 197049 0 None 4 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5175548 197049 0 None 4 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
2812 11551 101 None -39 34 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 11551 101 None -39 34 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
168280974 197642 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5184607 197642 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
21186186 207409 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL59942 207409 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
44336061 115398 0 None 56 2 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/jm058225d
CHEMBL320597 115398 0 None 56 2 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/jm058225d
10381889 113846 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL315772 113846 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(02)00796-5
10381889 113846 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL315772 113846 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 328 2 0 3 4.1 CN(C)CC1CC2c3ccccc3Cc3ccc(Cl)cc3N2O1 10.1016/s0960-894x(01)00721-1
10643697 127901 1 None 10 3 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL357448 127901 1 None 10 3 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
10450082 109091 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3Cc3ccccc3-4)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL303519 109091 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3Cc3ccccc3-4)CC2)nc1 10.1016/s0960-894x(98)00361-8
168294958 199183 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5207898 199183 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
168289523 198278 0 None 5 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5193761 198278 0 None 5 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
168285068 198362 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5195130 198362 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
127027237 146164 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793264 146164 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
168275717 196998 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5174731 196998 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5281787 200907 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 553 8 1 5 6.2 Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(-c2ccccc2)c1C(=O)NC1CCCCC1 10.1021/acs.jmedchem.1c00704
135398737 7745 93 None -13 90 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
38 7745 93 None -13 90 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
722 7745 93 None -13 90 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
CHEMBL42 7745 93 None -13 90 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
DB00363 7745 93 None -13 90 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981041x
72737730 121304 0 None 42 3 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335554 121304 0 None 42 3 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
2274 9947 58 None -56 31 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 9947 58 None -56 31 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 9947 58 None -56 31 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 9947 58 None -56 31 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 9947 58 None -56 31 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
155568411 182859 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4591118 182859 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
168281091 197850 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5187429 197850 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
21186148 208969 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4cnccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL60957 208969 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4cnccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
10108561 119721 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 295 2 0 4 2.8 CN(C)CC1CC2c3ccccc3Cc3ccncc3N2O1 10.1016/s0960-894x(02)00796-5
CHEMBL331077 119721 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 295 2 0 4 2.8 CN(C)CC1CC2c3ccccc3Cc3ccncc3N2O1 10.1016/s0960-894x(02)00796-5
155568867 182933 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 182933 0 None - 1 Human 4.6 pIC50 = 4.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
127028183 146094 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792532 146094 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
127032085 146166 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
CHEMBL3793266 146166 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
155513053 176477 0 None 6 3 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 176477 0 None 6 3 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
127027238 146189 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793709 146189 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL5282604 200944 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 657 7 1 5 6.5 CC(C)(C)NC(=O)Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2cc(Br)c(Br)cc21 10.1021/acs.jmedchem.1c00704
45482789 205704 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of dopamine D4.4 receptorInhibition of dopamine D4.4 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL584554 205704 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of dopamine D4.4 receptorInhibition of dopamine D4.4 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
127027905 146234 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3794079 146234 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
135418440 18840 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183663 18840 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL310311 18840 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
168296363 199296 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5209344 199296 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
10092041 172311 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccc2c(c1)C(CCCN1CCN(c3ccccc3OC)CC1)CCC2 10.1021/jm981041x
CHEMBL424125 172311 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccc2c(c1)C(CCCN1CCN(c3ccccc3OC)CC1)CCC2 10.1021/jm981041x
11730467 17800 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 17800 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
10688858 24867 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3cccc(Cl)c3)CC2)cc1 10.1021/jm990562x
CHEMBL1202223 24867 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3cccc(Cl)c3)CC2)cc1 10.1021/jm990562x
CHEMBL126793 24867 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3cccc(Cl)c3)CC2)cc1 10.1021/jm990562x
131396 213514 6 None 1 5 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL89934 213514 6 None 1 5 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
44304600 210043 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 344 3 0 5 3.7 c1cnc(N2CCN(Cc3cccc4c3oc3ccccc34)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL64622 210043 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 344 3 0 5 3.7 c1cnc(N2CCN(Cc3cccc4c3oc3ccccc34)CC2)nc1 10.1016/s0960-894x(98)00361-8
72737767 121298 4 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335540 121298 4 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
21186115 209485 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL61682 209485 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
9949655 210037 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL64597 210037 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
10666005 24724 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202211 24724 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126032 24724 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
10829708 24816 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202216 24816 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126509 24816 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
9799123 12391 0 None 35 2 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1021/jm058225d
CHEMBL107742 12391 0 None 35 2 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against dopamine receptor D4Inhibitory concentration against dopamine receptor D4
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1021/jm058225d
11726532 103801 0 None -2 4 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL26677 103801 0 None -2 4 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
10688859 24866 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990562x
CHEMBL1202222 24866 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990562x
CHEMBL126792 24866 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 344 4 0 2 4.4 Fc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1021/jm990562x
44363676 46810 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccc2c(c1)CC(NC(=O)CCN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL147897 46810 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccc2c(c1)CC(NC(=O)CCN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL2373210 46810 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 423 7 1 5 2.9 COc1ccc2c(c1)CC(NC(=O)CCN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
10572037 127800 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(Cc3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL2373204 127800 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(Cc3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL356581 127800 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 383 8 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(Cc3ccccc3OC)CC2)c1 10.1021/jm981041x
135612922 150479 2 None - 0 Human 4.5 pIC50 = 4.5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccc(O)cc3)CC2)nc2ccccc12 nan
CHEMBL3900329 150479 2 None - 0 Human 4.5 pIC50 = 4.5 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3ccc(O)cc3)CC2)nc2ccccc12 nan
19426635 212372 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
CHEMBL81485 212372 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 280 2 1 3 3.1 CNCC1CC2c3ccccc3Cc3ccccc3N2O1 10.1016/s0960-894x(01)00721-1
168271259 197294 0 None 2 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179459 197294 0 None 2 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
163322331 198994 3 None 8 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5204764 198994 3 None 8 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
10688561 123645 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 4 0 2 4.6 Cc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202210 123645 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 4 0 2 4.6 Cc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL338183 123645 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 4 0 2 4.6 Cc1cc(Cl)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
4797946 177203 7 None 165 3 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 177203 7 None 165 3 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3117 214620 103 None -2 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 214620 103 None -2 16 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
168268918 196786 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
CHEMBL5171398 196786 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
135398737 7745 93 None -13 90 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
38 7745 93 None -13 90 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
722 7745 93 None -13 90 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
CHEMBL42 7745 93 None -13 90 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
DB00363 7745 93 None -13 90 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2013.03.016
127053222 146147 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3793072 146147 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
168270455 196812 0 None 1 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5171772 196812 0 None 1 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
2 10035 23 None -2 28 Human 7.5 pIC50 = 7.5 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00704
54562 10035 23 None -2 28 Human 7.5 pIC50 = 7.5 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00704
CHEMBL240773 10035 23 None -2 28 Human 7.5 pIC50 = 7.5 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00704
135 9310 43 None - 56 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
1796 9310 43 None - 56 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
4184 9310 43 None - 56 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
CHEMBL6437 9310 43 None - 56 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
DB06148 9310 43 None - 56 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1016/s0960-894x(01)00721-1
11071079 117370 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL325516 117370 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 496 9 0 3 6.0 O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
168294968 199198 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208124 199198 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
127028505 146111 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792731 146111 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
4223 10764 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
6918314 10764 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
7427 10764 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
CHEMBL439849 10764 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
DB06684 10764 94 None - 3 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat dopamine D4 receptorInhibition of rat dopamine D4 receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
168291477 198660 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5199649 198660 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5281830 200911 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 561 9 1 5 6.1 Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(-c2ccccc2)c1C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00704
19964406 121293 2 None 75 2 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335535 121293 2 None 75 2 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
53320009 63437 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
CHEMBL1642116 63437 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 435 3 0 5 3.4 CN1CCN(c2ccc3c(c2)N(S(=O)(=O)c2ccc4ccccc4c2)CCC3=O)CC1 10.1016/j.bmcl.2010.12.007
72737772 121299 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335541 121299 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
10782111 24659 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL1202217 24659 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL125910 24659 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
127029388 146117 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792803 146117 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
45361874 176800 2 None 48 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 176800 2 None 48 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168277394 197180 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5177641 197180 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
127031516 146087 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792438 146087 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
92988697 146245 1 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794199 146245 1 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
92984956 146258 1 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794363 146258 1 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
46885213 15232 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of dopamine D4 (receptor)Inhibition of dopamine D4 (receptor)
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
CHEMBL1093802 15232 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of dopamine D4 (receptor)Inhibition of dopamine D4 (receptor)
ChEMBL 549 8 2 5 2.2 O=C(CNC(=O)c1cccc(C(F)(F)F)c1)N[C@@H]1CCN(CCN2CCN(C(=O)c3ccccc3F)CC2)C1 10.1016/j.bmcl.2010.02.072
155530763 178348 0 None 9 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 178348 0 None 9 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
127031833 146173 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
CHEMBL3793347 146173 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
54477 91428 36 None -14 22 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm990562x
CHEMBL22242 91428 36 None -14 22 Human 5.4 pIC50 = 5.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm990562x
72737725 121303 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335545 121303 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
127029387 146185 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793612 146185 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
72737734 121300 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
CHEMBL3335542 121300 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
10034684 76182 69 None 18 2 Human 4.4 pIC50 = 4.4 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
CHEMBL19331 76182 69 None 18 2 Human 4.4 pIC50 = 4.4 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
155562395 182727 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 182727 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
54577891 73349 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
inhibition of dopamine D4 receptor by competition binding assayinhibition of dopamine D4 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL1852516 73349 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
inhibition of dopamine D4 receptor by competition binding assayinhibition of dopamine D4 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
CHEMBL3216758 73349 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
inhibition of dopamine D4 receptor by competition binding assayinhibition of dopamine D4 receptor by competition binding assay
ChEMBL 471 6 1 5 4.3 Cc1nc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c(C)n1-c1ccccc1 10.1021/jm200682b
17888044 209702 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL62829 209702 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
10832895 127772 7 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1ccccc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm981041x
CHEMBL356358 127772 7 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 369 7 1 5 2.3 COc1ccccc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1021/jm981041x
135398737 7745 93 None -13 90 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
38 7745 93 None -13 90 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
722 7745 93 None -13 90 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
CHEMBL42 7745 93 None -13 90 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
DB00363 7745 93 None -13 90 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
135398737 7745 93 None -13 90 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
38 7745 93 None -13 90 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
722 7745 93 None -13 90 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
CHEMBL42 7745 93 None -13 90 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
DB00363 7745 93 None -13 90 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant Dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2016.03.006
127031518 146177 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793389 146177 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
127029995 146275 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3794529 146275 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
3303 9024 46 None 1 15 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
5311200 9024 46 None 1 15 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
CHEMBL267014 9024 46 None 1 15 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
155511803 176384 0 None 229 2 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4436479 176384 0 None 229 2 Human 4.4 pIC50 = 4.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
155536720 178966 0 None 77 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 178966 0 None 77 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
168270563 196729 0 None -1 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170381 196729 0 None -1 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
11035765 16660 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 359 6 2 6 3.3 Oc1nc2ccccc2n1CCCNCc1cc2c(cc1Cl)OCO2 10.1021/jm010878g
CHEMBL114280 16660 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 359 6 2 6 3.3 Oc1nc2ccccc2n1CCCNCc1cc2c(cc1Cl)OCO2 10.1021/jm010878g
11793971 24738 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 376 4 1 3 4.6 Oc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL1202202 24738 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 376 4 1 3 4.6 Oc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL126126 24738 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 376 4 1 3 4.6 Oc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
109030515 182764 1 None 12 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 182764 1 None 12 3 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168292271 198668 0 None 5 2 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5199815 198668 0 None 5 2 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
168295019 199278 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5209079 199278 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
10668173 26215 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL1202206 26215 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
CHEMBL129556 26215 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 390 5 0 3 4.9 COc1ccc([C@H]2C[C@@H]2CN2CCN(c3ccc(Cl)cc3Cl)CC2)cc1 10.1021/jm990562x
127053214 146127 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3792923 146127 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
155515982 176789 0 None 6 17 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 176789 0 None 6 17 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
127031829 146206 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793890 146206 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
127028182 146240 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
CHEMBL3794158 146240 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
127029386 146175 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793375 146175 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
44363656 42249 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccc2c(c1)CC(NC(=O)CN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL143835 42249 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccc2c(c1)CC(NC(=O)CN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
CHEMBL2373208 42249 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccc2c(c1)CC(NC(=O)CN1CCN(c3ccccc3OC)CC1)CC2 10.1021/jm981041x
71717830 92758 0 None 9 2 Human 4.3 pIC50 = 4.3 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
CHEMBL2303762 92758 0 None 9 2 Human 4.3 pIC50 = 4.3 Binding
Inhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptorInhibitory concentration against binding of [3H]spiperone to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
168275515 197284 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179340 197284 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
10851217 125303 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 292 4 0 2 3.6 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL341497 125303 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 292 4 0 2 3.6 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccc3)CC2)cc1 10.1021/jm990562x
44304314 109469 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3-c3ccccc3C4)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL304692 109469 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 342 3 0 4 3.4 c1cnc(N2CCN(Cc3cccc4c3-c3ccccc3C4)CC2)nc1 10.1016/s0960-894x(98)00361-8
155559617 181663 0 None 9 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 181663 0 None 9 3 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
135514603 210893 14 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 474 2 1 7 4.0 CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL70319 210893 14 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 474 2 1 7 4.0 CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
3303 9024 46 None 1 15 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
5311200 9024 46 None 1 15 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
CHEMBL267014 9024 46 None 1 15 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00361-8
5615 10671 8 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
5781 10671 8 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
CHEMBL1179189 10671 8 None - 1 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
1353 8692 93 None -3 85 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
3559 8692 93 None -3 85 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
86 8692 93 None -3 85 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
CHEMBL54 8692 93 None -3 85 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
DB00502 8692 93 None -3 85 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm990562x
9901894 170195 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL1202220 170195 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL419610 170195 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
11301655 6988 37 None 245 4 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
8441 6988 37 None 245 4 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
CHEMBL127257 6988 37 None 245 4 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assayIn vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
127031515 146212 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL3793910 146212 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5274672 200604 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 527 7 1 5 5.7 Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc(-c2ccccc2)c1C(=O)NC(C)(C)C 10.1021/acs.jmedchem.1c00704
135620651 151286 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3cccc(O)c3)CC2)nc2ccccc12 nan
CHEMBL3906995 151286 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.Receptor Binding Assay: Determination of binding to D4.4 receptor was performed using [3H]-YM-09151-2 (70-87 Ci/mmol, 0.3 nM), as a radioligand, in the presence of various concentrations of the tested compound. Reactions were carried out in 50 mM TRIS-HCl (pH 7.4) containing 5 mM MgCl2, 5 mM EDTA, 5 mM KCl and 1.5 mM CaCl2, for 60 minutes at 22° C. The reaction was terminated by rapid vacuum filtration onto glass fiber filters.
ChEMBL 336 3 2 5 2.0 O=c1[nH]c(CN2CCN(c3cccc(O)c3)CC2)nc2ccccc12 nan
135398737 7745 93 None -13 90 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
38 7745 93 None -13 90 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
722 7745 93 None -13 90 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
CHEMBL42 7745 93 None -13 90 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
DB00363 7745 93 None -13 90 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
127053220 146145 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793062 146145 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
11005810 17238 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 17238 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL5278254 200750 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 497 6 1 5 3.0 CN1CCN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)C(C(=O)NC(C)(C)C)C1 10.1021/acs.jmedchem.1c00704
51003551 63444 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
CHEMBL1642123 63444 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cells
ChEMBL 449 3 0 5 3.8 CC1CC(=O)c2c(N3CCN(C)CC3)cccc2N1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2010.12.007
127031515 146212 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793910 146212 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
1353 8692 93 None -3 85 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 8692 93 None -3 85 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 8692 93 None -3 85 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 8692 93 None -3 85 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 8692 93 None -3 85 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
10803754 24879 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 294 4 0 4 2.4 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ncccn3)CC2)cc1 10.1021/jm990562x
CHEMBL1203257 24879 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 294 4 0 4 2.4 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ncccn3)CC2)cc1 10.1021/jm990562x
CHEMBL126847 24879 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 294 4 0 4 2.4 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ncccn3)CC2)cc1 10.1021/jm990562x
21186102 107554 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL292943 107554 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 5 0 5 3.5 COc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
10049758 211424 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL73589 211424 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
137640201 163740 2 None 177 13 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 163740 2 None 177 13 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
168287735 198583 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5198353 198583 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5266395 200257 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 486 7 0 4 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)N1C=CN(Cc2ccccc2)C(=O)C1 10.1021/acs.jmedchem.1c00704
127031519 146101 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792638 146101 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127053221 146109 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3792728 146109 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
127032383 146181 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793438 146181 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
135398737 7745 93 None -13 90 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
38 7745 93 None -13 90 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
722 7745 93 None -13 90 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
CHEMBL42 7745 93 None -13 90 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
DB00363 7745 93 None -13 90 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
1212 8443 50 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -77 65 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
127032082 146095 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792541 146095 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
21186124 108989 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 347 4 0 3 4.2 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL302904 108989 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 347 4 0 3 4.2 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
9949655 210037 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
CHEMBL64597 210037 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 336 4 0 5 3.5 c1cnc(N2CCN(Cc3cccc(-c4ccsc4)c3)CC2)nc1 10.1016/s0960-894x(98)00361-8
10617133 24771 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 5 0 3 3.8 COc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202214 24771 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 5 0 3 3.8 COc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126269 24771 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 340 5 0 3 3.8 COc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
9820304 108846 0 None 12 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL1204116 108846 0 None 12 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL302075 108846 0 None 12 2 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
1353 8692 93 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
3559 8692 93 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
86 8692 93 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
CHEMBL54 8692 93 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
DB00502 8692 93 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
10236758 122550 5 None 208 13 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 122550 5 None 208 13 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
1353 8692 93 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
3559 8692 93 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
86 8692 93 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
CHEMBL54 8692 93 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
DB00502 8692 93 None -3 85 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
10385977 104106 0 None -5 2 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1021/jm981041x
CHEMBL26929 104106 0 None -5 2 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1021/jm981041x
CHEMBL5270832 200434 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 523 7 1 5 3.5 CN1CCN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)C(C(=O)NC2CCCCC2)C1 10.1021/acs.jmedchem.1c00704
2247 7293 81 None -63 42 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 7293 81 None -63 42 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 7293 81 None -63 42 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 7293 81 None -63 42 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 7293 81 None -63 42 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
127031508 146159 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793169 146159 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
155552185 180840 0 None 2 16 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 180840 0 None 2 16 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assayAntagonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as inhibition of quinpirole-induced beta-arrestin2 recruitment preincubated for 30 mins followed by quinpirole addition and further incubated for 6 hrs by Path-Hunter assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
127053217 146096 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792556 146096 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
45278882 14224 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086756 14224 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 512 9 1 4 6.1 CCCn1c(-c2ccccc2)cc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1C 10.1016/j.bmcl.2010.01.093
168274850 196934 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5173767 196934 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
168274755 197421 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5181334 197421 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
127032083 146225 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793996 146225 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
72198754 97655 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of dopamine D4 receptor (unknown origin)Inhibition of dopamine D4 receptor (unknown origin)
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
CHEMBL2392349 97655 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of dopamine D4 receptor (unknown origin)Inhibition of dopamine D4 receptor (unknown origin)
ChEMBL 443 8 0 4 4.8 COc1ccccc1N1CCN(CCCCCN2Cc3ccc4ccccc4c3C2=O)CC1 10.1016/j.ejmech.2013.01.044
10905740 117447 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 413 3 1 6 2.9 O=c1[nH]c2ccccc2n(C2CCN(Cc3cc4c(cc3Cl)OCO4)CC2)c1=O 10.1021/jm010878g
CHEMBL325945 117447 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 413 3 1 6 2.9 O=c1[nH]c2ccccc2n(C2CCN(Cc3cc4c(cc3Cl)OCO4)CC2)c1=O 10.1021/jm010878g
CHEMBL5266508 200263 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 497 6 2 5 2.1 CC(C)(C)NC(=O)C1C(=O)NCCN1C(=O)CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00704
10615990 124083 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 324 4 0 2 4.1 Cc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202209 124083 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 324 4 0 2 4.1 Cc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL339674 124083 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 324 4 0 2 4.1 Cc1cc(F)ccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
127053219 146242 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794174 146242 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL5269858 200391 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 523 7 2 5 2.7 O=C1NCCN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)C1C(=O)NC1CCCCC1 10.1021/acs.jmedchem.1c00704
15840855 108866 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL302183 108866 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
21186186 207409 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL59942 207409 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
21186138 209477 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cncc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL61657 209477 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccc(-c2cncc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
21186115 209485 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL61682 209485 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccccc4F)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
9797162 85116 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(CC3CC3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL2092961 85116 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(CC3CC3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL2109988 85116 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(CC3CC3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
10501113 43321 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 399 8 1 6 2.3 COc1ccc(OC)c(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL144811 43321 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 399 8 1 6 2.3 COc1ccc(OC)c(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm981041x
CHEMBL5273880 200562 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 501 7 1 5 5.0 CC(C)(C)NC(=O)Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2ccccc21 10.1021/acs.jmedchem.1c00704
10762827 128705 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
CHEMBL2373207 128705 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
CHEMBL359051 128705 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(Cc3ccc(Cl)cc3)CC2)c1 10.1021/jm981041x
10411988 28182 0 None -29 2 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL131482 28182 0 None -29 2 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human Dopamine receptor D4.2 in CHO cellsInhibitory concentration against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
11113605 17279 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL116735 17279 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 480 9 0 2 5.8 O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
10496095 123608 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL1202224 123608 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
CHEMBL337983 123608 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 322 5 0 3 3.6 COc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1 10.1021/jm990562x
155536815 178986 0 None 33 3 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
CHEMBL4473792 178986 0 None 33 3 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
10739483 43395 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 395 6 0 6 4.2 COc1cccc(-c2csc(CN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL144868 43395 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 395 6 0 6 4.2 COc1cccc(-c2csc(CN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL2373206 43395 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 395 6 0 6 4.2 COc1cccc(-c2csc(CN3CCN(c4ccccc4OC)CC3)n2)c1 10.1021/jm981041x
CHEMBL5268231 200332 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 468 8 1 4 3.8 CN(CC(=O)NC1CCCCC1)C(=O)CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00704
127028181 146227 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794013 146227 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10885636 117793 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 117793 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
155563301 182029 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 182029 0 None - 1 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assayAntagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
5615 10671 8 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
5781 10671 8 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
CHEMBL1179189 10671 8 None - 1 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 10.1016/s0960-894x(98)00361-8
21186098 107319 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL291380 107319 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1ccccc1-c1cccc(CN2CCN(c3ncccn3)CC2)c1 10.1016/s0960-894x(98)00361-8
21186192 107379 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccc(F)cc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL291824 107379 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 365 4 0 3 4.3 Fc1ccc(-c2cncc(CN3CCN(c4ccc(F)cc4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
10615684 24813 0 None 4 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL1202208 24813 0 None 4 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
CHEMBL126493 24813 0 None 4 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 320 4 0 2 4.2 Cc1ccc(N2CCN(C[C@@H]3C[C@H]3c3ccccc3)CC2)c(C)c1 10.1021/jm990562x
9967140 24839 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202215 24839 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126633 24839 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1ccccc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
127032384 146154 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793137 146154 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10568183 24750 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL1202221 24750 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
CHEMBL126182 24750 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 326 4 0 2 4.3 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1 10.1021/jm990562x
44363675 126031 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccccc1N1CCN(CC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
CHEMBL2373209 126031 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccccc1N1CCN(CC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
CHEMBL343620 126031 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.In vitro binding affinity at human cloned Dopamine receptor D4.2 by [3H]YM-09151-2 displacement.
ChEMBL 409 6 1 5 2.5 COc1ccccc1N1CCN(CC(=O)NC2CCc3c(cccc3OC)C2)CC1 10.1021/jm981041x
168286314 198438 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5196213 198438 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5283891 201012 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 531 8 2 5 2.5 O=C1NCCN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)C1C(=O)NCc1ccccc1 10.1021/acs.jmedchem.1c00704
15840855 108866 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
CHEMBL302183 108866 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 349 4 0 5 3.0 Fc1ccc(-c2cncc(CN3CCN(c4ncccn4)CC3)c2)cc1 10.1016/s0960-894x(98)00361-8
17888044 209702 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
CHEMBL62829 209702 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperoneBinding affinity to cloned human Dopamine receptor D4 expressed in CHO cells using [3H]spiperone
ChEMBL 348 4 0 4 3.6 Fc1cccc(-c2cccc(CN3CCN(c4ncccn4)CC3)c2)c1 10.1016/s0960-894x(98)00361-8
10808230 24833 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1ccc(Cl)cc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL1202205 24833 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1ccc(Cl)cc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
CHEMBL126604 24833 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 356 5 0 3 4.3 COc1ccc(Cl)cc1N1CCN(C[C@H]2C[C@@H]2c2ccccc2)CC1 10.1021/jm990562x
9820304 108846 0 None 12 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL1204116 108846 0 None 12 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
CHEMBL302075 108846 0 None 12 2 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1021/jm990562x
10761040 125248 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1Cl 10.1021/jm990562x
CHEMBL1202213 125248 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1Cl 10.1021/jm990562x
CHEMBL341310 125248 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 360 4 0 2 4.9 Clc1cccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c1Cl 10.1021/jm990562x
14925759 164817 6 None 18 13 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 164817 6 None 18 13 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL5278601 200766 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 691 9 1 5 6.9 O=C(Cn1c(CCCN2CCN(c3cccc(Cl)c3Cl)CC2)nc2cc(Br)c(Br)cc21)NCc1ccccc1 10.1021/acs.jmedchem.1c00704
CHEMBL5273430 200542 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysisPartial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis
ChEMBL 531 8 1 5 3.4 CN1CCN(C(=O)CCCN2CCN(c3cccc(Cl)c3Cl)CC2)C(C(=O)NCc2ccccc2)C1 10.1021/acs.jmedchem.1c00704
127029389 146221 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793984 146221 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
3303 9024 46 None 1 15 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
5311200 9024 46 None 1 15 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
CHEMBL267014 9024 46 None 1 15 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assayAntagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
3198 212292 76 None -26 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 212292 76 None -26 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 212292 76 None -26 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
10948527 118132 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 365 3 1 5 2.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3c(c1)OCO3)CC2 10.1021/jm010878g
CHEMBL326962 118132 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D4.4Inhibition of human dopamine receptor D4.4
ChEMBL 365 3 1 5 2.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3c(c1)OCO3)CC2 10.1021/jm010878g
135492584 18105 0 None 95 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179503 18105 0 None 95 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80645 18105 0 None 95 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
135481864 19122 0 None 112 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1185415 19122 0 None 112 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL412665 19122 0 None 112 3 Human 7.0 pIC50 = 7.0 Binding
Inhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptorInhibition of 333 nM dopamine stimulated GTP binding in CHO cells expressing human D4 receptor
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
168284020 198032 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5190239 198032 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
10780076 24777 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 293 4 0 3 3.0 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccn3)CC2)cc1 10.1021/jm990562x
CHEMBL1203260 24777 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 293 4 0 3 3.0 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccn3)CC2)cc1 10.1021/jm990562x
CHEMBL126318 24777 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligandBinding affinity to dopamine receptor D4 cloned from human, using [3H]- YM09151 as competitive ligand
ChEMBL 293 4 0 3 3.0 c1ccc([C@H]2C[C@@H]2CN2CCN(c3ccccn3)CC2)cc1 10.1021/jm990562x
127031497 146269 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794469 146269 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
4452 9538 19 None -7 18 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/acs.jmedchem.9b00412
983 9538 19 None -7 18 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/acs.jmedchem.9b00412
CHEMBL20734 9538 19 None -7 18 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D4 receptor expressed in CHOK1 cells assessed as inhibition of lisuride-induced beta arrestin2 recruitment preincubated for 30 mins followed by lisuride-stimulation and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/acs.jmedchem.9b00412
45278805 14222 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 484 7 1 4 5.2 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1C 10.1016/j.bmcl.2010.01.093
CHEMBL1086754 14222 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 484 7 1 4 5.2 Cc1c(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(-c2ccccc2)n1C 10.1016/j.bmcl.2010.01.093
164612037 192156 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 192156 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 199747 0 None -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 199747 0 None -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 199747 0 None -5 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 199798 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 199798 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 199798 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 199810 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 199810 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 199810 0 None -1 20 Human 10.1 pKd = 10.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from human D4.4 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD4.4R-ELuc incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
4452 9538 19 None -7 18 Human 9.7 pKd = 9.7 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm9601720
983 9538 19 None -7 18 Human 9.7 pKd = 9.7 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm9601720
CHEMBL20734 9538 19 None -7 18 Human 9.7 pKd = 9.7 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1021/jm9601720
9849682 101727 0 None -602 10 Human 6.9 pKd = 6.9 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254500 101727 0 None -602 10 Human 6.9 pKd = 6.9 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
10162564 19312 0 None -218 8 Human 6.9 pKd = 6.9 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186652 19312 0 None -218 8 Human 6.9 pKd = 6.9 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL473763 19312 0 None -218 8 Human 6.9 pKd = 6.9 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
3251 10844 58 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
5684 10844 58 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
80 10844 58 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
CHEMBL31354 10844 58 None -43 12 Human 8.6 pKd = 8.6 Binding
Binding affinity to D4 receptor (unknown origin) assessed as dissociation constantBinding affinity to D4 receptor (unknown origin) assessed as dissociation constant
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/acs.jmedchem.2c00633
11724450 130626 4 None - 1 Human 8.4 pKd = 8.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 130626 4 None - 1 Human 8.4 pKd = 8.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 130626 4 None - 1 Human 8.4 pKd = 8.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
17955460 183554 0 None -630 9 Human 6.3 pKd = 6.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL460542 183554 0 None -630 9 Human 6.3 pKd = 6.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
2030 10444 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2009.01.072
5311377 10444 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2009.01.072
CHEMBL251541 10444 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2009.01.072
2030 10444 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
5311377 10444 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
CHEMBL251541 10444 10 None -7 10 Human 8.3 pKd = 8.3 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
44447073 101325 0 None -208 10 Human 7.1 pKd = 7.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251835 101325 0 None -208 10 Human 7.1 pKd = 7.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
11729231 56384 0 None 1584 3 Human 10.7 pKi = 10.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 407 6 1 4 3.6 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL156599 56384 0 None 1584 3 Human 10.7 pKi = 10.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 407 6 1 4 3.6 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
11131951 56695 1 None 363 4 Human 10.6 pKi = 10.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm020952a
CHEMBL156845 56695 1 None 363 4 Human 10.6 pKi = 10.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm020952a
4257 85030 30 None - 1 Human 10.5 pKi = 10.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 10.1016/j.ejmech.2019.111569
CHEMBL2106650 85030 30 None - 1 Human 10.5 pKi = 10.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 10.1016/j.ejmech.2019.111569
3504099 98935 6 None 3388 3 Human 10.5 pKi = 10.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 335 5 1 3 3.9 CCOc1ccccc1N1CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420894 98935 6 None 3388 3 Human 10.5 pKi = 10.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 335 5 1 3 3.9 CCOc1ccccc1N1CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
10948748 57230 0 None 676 2 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm020952a
CHEMBL157322 57230 0 None 676 2 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm020952a
3626837 214094 11 None 125 4 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL93403 214094 11 None 125 4 Human 10.4 pKi = 10.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
3626837 214094 11 None 125 4 Human 10.4 pKi = 10.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL93403 214094 11 None 125 4 Human 10.4 pKi = 10.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
16363 7383 53 None -1 7 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
312 7383 53 None -1 7 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
9215 7383 53 None -1 7 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
CHEMBL297302 7383 53 None -1 7 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
DB12867 7383 53 None -1 7 Human 10.2 pKi = 10.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand displacement assayBinding affinity to human dopamine D4 receptor by radioligand displacement assay
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1016/j.bmc.2016.06.011
2470 10425 50 None -20 58 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
3300 10425 50 None -20 58 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
5265 10425 50 None -20 58 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
99 10425 50 None -20 58 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
CHEMBL267930 10425 50 None -20 58 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2013.01.025
72901200 126555 25 None 154 4 Human 9.7 pKi = 9.7 Binding
Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5212743
CHEMBL3480577 126555 25 None 154 4 Human 9.7 pKi = 9.7 Binding
Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4Selectivity interaction (BRET-Gi dissociation assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5212743
11090403 126322 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 389 6 1 4 3.4 COc1cccc(C(=O)NCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL345848 126322 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 389 6 1 4 3.4 COc1cccc(C(=O)NCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
9977532 117968 1 None 6 4 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL326454 117968 1 None 6 4 Human 9.6 pKi = 9.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
11574902 85225 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
CHEMBL211164 85225 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
155515982 176789 0 None 6 17 Human 9.6 pKi = 9.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 176789 0 None 6 17 Human 9.6 pKi = 9.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
11574902 85225 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1021/jm060166w
CHEMBL211164 85225 0 None 537 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1021/jm060166w
11036114 57295 0 None 134 2 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)c1 10.1021/jm020952a
CHEMBL157388 57295 0 None 134 2 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)c1 10.1021/jm020952a
17449900 146320 13 None 23 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 146320 13 None 23 6 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
10733406 26213 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL129534 26213 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
10733406 26213 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
CHEMBL129534 26213 0 None 70 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
10546540 214016 0 None 288 3 Human 9.5 pKi = 9.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
CHEMBL92859 214016 0 None 288 3 Human 9.5 pKi = 9.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
11583188 146060 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
CHEMBL379125 146060 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1016/j.ejmech.2019.111569
2470 10425 50 None -20 58 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
3300 10425 50 None -20 58 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
5265 10425 50 None -20 58 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
99 10425 50 None -20 58 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
CHEMBL267930 10425 50 None -20 58 Human 9.5 pKi = 9.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm049612a
5041 10067 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1016/j.ejmech.2020.113141
981 10067 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1016/j.ejmech.2020.113141
CHEMBL4096543 10067 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from D4 (unknown origin) receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1016/j.ejmech.2020.113141
11583188 146060 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
CHEMBL379125 146060 0 None 218 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
5041 10067 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
981 10067 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
CHEMBL4096543 10067 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
5041 10067 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.8b00265
981 10067 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.8b00265
CHEMBL4096543 10067 6 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.8b00265
49788939 25031 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 368 5 1 5 2.5 O=C(NCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)cc1 10.1021/jm100925m
CHEMBL1270323 25031 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 368 5 1 5 2.5 O=C(NCCN1CCN(c2noc3ccccc23)CC1)c1ccc(F)cc1 10.1021/jm100925m
10780510 26269 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1016/j.bmcl.2005.02.012
CHEMBL129927 26269 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1016/j.bmcl.2005.02.012
10780510 26269 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1021/jm970422s
CHEMBL129927 26269 0 None 208 3 Human 9.5 pKi = 9.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2)cc1C 10.1021/jm970422s
44400585 75430 0 None 26 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 75430 0 None 26 5 Human 9.4 pKi = 9.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
21219157 105676 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Binding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cellsBinding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1021/jm030836n
CHEMBL279247 105676 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Binding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cellsBinding affinity of compound towards human Dopamine receptor D4 by displacing [125I]-iodosulpiride expressed in CHO cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1021/jm030836n
21219157 105676 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL279247 105676 0 None 15 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1nn(C2CCN(Cc3ccccc3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0305669
3716121 90856 16 None 70 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.ejmech.2020.113141
CHEMBL2207643 90856 16 None 70 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.ejmech.2020.113141
3716121 90856 16 None 70 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207643 90856 16 None 70 5 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
168287284 199714 0 None 316 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5198170 199714 0 None 316 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222300 199714 0 None 316 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2[N+](=O)[O-])CC1 10.1021/acs.jmedchem.2c00840
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(99)00025-6
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(99)00025-6
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(99)00025-6
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmcl.2004.09.046
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmcl.2004.09.046
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmcl.2004.09.046
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0002432
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0002432
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0002432
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2008.12.054
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2008.12.054
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2008.12.054
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2020.113141
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2020.113141
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2020.113141
3303 9024 46 None -1 15 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2014.04.026
5311200 9024 46 None -1 15 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2014.04.026
CHEMBL267014 9024 46 None -1 15 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2014.04.026
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human Dopamine receptor D4In vitro binding affinity to human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human Dopamine receptor D4In vitro binding affinity to human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity to human Dopamine receptor D4In vitro binding affinity to human Dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm981041x
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm981041x
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm981041x
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.7b00151
44412482 84934 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1021/jm0611152
CHEMBL210404 84934 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1021/jm0611152
44412482 84934 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210404 84934 0 None 79 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1016/j.bmcl.2006.02.075
2470 10425 50 None -20 58 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
3300 10425 50 None -20 58 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
5265 10425 50 None -20 58 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
99 10425 50 None -20 58 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
CHEMBL267930 10425 50 None -20 58 Human 9.4 pKi = 9.4 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.7b01248
44436598 156074 0 None 112 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL394473 156074 0 None 112 4 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
2470 10425 50 None -20 58 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
3300 10425 50 None -20 58 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
5265 10425 50 None -20 58 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
99 10425 50 None -20 58 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
CHEMBL267930 10425 50 None -20 58 Human 9.4 pKi = 9.4 Binding
Inhibition of D4 receptor (unknown origin)Inhibition of D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/acs.jmedchem.9b00412
10660814 25644 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL128232 25644 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1016/j.bmcl.2005.02.012
10667579 214165 0 None 2818 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm991029k
CHEMBL93832 214165 0 None 2818 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(Cl)c2)CC1 10.1021/jm991029k
10660814 25644 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
CHEMBL128232 25644 2 None 134 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1cccc(OCCNCCCOc2ccccc2)c1 10.1021/jm970422s
119570 9933 96 None -6 39 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 9933 96 None -6 39 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 9933 96 None -6 39 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 9933 96 None -6 39 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 9933 96 None -6 39 Human 9.3 pKi = 9.3 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL5285358 201073 0 None 7413 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 334 4 2 4 3.3 O/N=C/c1c(CN2CCN(c3ccccc3)CC2)[nH]c2ccccc12 10.1016/j.ejmech.2020.113141
6603897 9027 22 None -5 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
978 9027 22 None -5 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
CHEMBL60518 9027 22 None -5 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm9600712
168268758 199544 0 None 107 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5172201 199544 0 None 107 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221189 199544 0 None 107 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
10708280 25722 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128647 25722 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
10450892 28643 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1021/jm970422s
CHEMBL131997 28643 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1021/jm970422s
9995904 37993 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1016/j.ejmech.2020.113141
CHEMBL140099 37993 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1016/j.ejmech.2020.113141
9995904 37993 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140099 37993 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
9995904 37993 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060166w
CHEMBL140099 37993 4 None 1047 5 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060166w
44400674 131967 0 None -1 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 131967 0 None -1 5 Human 9.3 pKi = 9.3 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
10708280 25722 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128647 25722 1 None 323 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10450892 28643 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1016/j.bmcl.2005.02.012
CHEMBL131997 28643 0 None 7 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCNCCCOc2ccccc2)cc1Cl 10.1016/j.bmcl.2005.02.012
10315310 29655 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL132884 29655 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10315310 29655 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL132884 29655 0 None 58 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
11655570 86501 0 None 173 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 462 4 0 5 3.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(I)c3n2)CC1 10.1021/jm060166w
CHEMBL211590 86501 0 None 173 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 462 4 0 5 3.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(I)c3n2)CC1 10.1021/jm060166w
32224 213684 6 None 4 3 Human 9.3 pKi = 9.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00004a016
CHEMBL90882 213684 6 None 4 3 Human 9.3 pKi = 9.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00004a016
32224 213684 6 None 4 3 Human 9.3 pKi = 9.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL90882 213684 6 None 4 3 Human 9.3 pKi = 9.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3ccccc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
3303 9024 46 None 1 15 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
5311200 9024 46 None 1 15 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
CHEMBL267014 9024 46 None 1 15 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
44326285 118319 0 None 2 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL327984 118319 0 None 2 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
9888765 196397 1 None 3 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned dopamine D4.4 receptorBinding affinity to human cloned dopamine D4.4 receptor
ChEMBL 427 7 1 5 5.1 Nc1nc(-c2ccc(F)cc2)c([C@@H]2CCN(CCCC(=O)c3ccc(F)cc3)C2)s1 10.1016/j.bmc.2008.02.091
CHEMBL514848 196397 1 None 3 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human cloned dopamine D4.4 receptorBinding affinity to human cloned dopamine D4.4 receptor
ChEMBL 427 7 1 5 5.1 Nc1nc(-c2ccc(F)cc2)c([C@@H]2CCN(CCCC(=O)c3ccc(F)cc3)C2)s1 10.1016/j.bmc.2008.02.091
155552185 180840 0 None 2 16 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 180840 0 None 2 16 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
155559617 181663 0 None 9 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4563944 181663 0 None 9 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
10522613 213737 0 None 389 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91229 213737 0 None 389 2 Human 9.3 pKi = 9.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCc2ccccc2)CC1 10.1021/jm991029k
44419065 91098 0 None 56 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 317 4 0 3 4.3 c1ccc(C2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL221600 91098 0 None 56 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 317 4 0 3 4.3 c1ccc(C2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
11983282 145721 0 None 56 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 145721 0 None 56 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
9950165 213728 0 None 93 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91162 213728 0 None 93 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
3303 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
5311200 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
CHEMBL267014 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
3303 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
5311200 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
CHEMBL267014 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.ejmech.2022.114840
44400519 139907 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 139907 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
168268758 199544 0 None 107 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5172201 199544 0 None 107 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221189 199544 0 None 107 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2Cl)CC1 10.1021/acs.jmedchem.2c00840
9977022 199670 0 None 131 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5189614 199670 0 None 131 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222031 199670 0 None 131 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
3303 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0611152
5311200 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0611152
CHEMBL267014 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm0611152
3303 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
5311200 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
CHEMBL267014 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
3303 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
5311200 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
CHEMBL267014 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
10783358 46441 4 None 42 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm020952a
CHEMBL147483 46441 4 None 42 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 340 6 1 5 1.6 COc1cccc(C(=O)NCCN2CCN(c3ccccn3)CC2)c1 10.1021/jm020952a
11676195 201927 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL550222 201927 0 None 1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
44400626 77177 0 None 38 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 77177 0 None 38 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
10547607 213725 0 None 1380 2 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
CHEMBL91155 213725 0 None 1380 2 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1cccc(CN2CCC(n3c(O)nc(-c4ccccc4)c3C)CC2)c1 10.1021/jm991029k
CHEMBL5272162 200490 0 None 3162 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 321 4 2 3 3.0 OCc1[nH]c2ccccc2c1CN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2020.113141
168285556 199696 0 None 2454 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 199696 0 None 2454 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 199696 0 None 2454 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
11057969 40045 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm049612a
CHEMBL141845 40045 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm049612a
11057969 40045 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL141845 40045 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
10669042 114921 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 405 5 2 4 4.2 CNc1cc(OC)c(C(=O)N[C@H]2CCN(C3C4CCCC3CCC4)C2)cc1Cl 10.1021/jm9601720
CHEMBL319597 114921 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 405 5 2 4 4.2 CNc1cc(OC)c(C(=O)N[C@H]2CCN(C3C4CCCC3CCC4)C2)cc1Cl 10.1021/jm9601720
168268850 199563 0 None 741 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5179930 199563 0 None 741 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221350 199563 0 None 741 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.2c00840
11057969 40045 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
CHEMBL141845 40045 0 None 223 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
25072633 166000 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 166000 0 None 1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
168268839 199560 0 None 30 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5177462 199560 0 None 30 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221334 199560 0 None 30 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.2c00840
792584 98927 7 None 58 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 297 5 0 4 2.8 CCOc1ccccc1N1CCN(Cc2cccnc2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420779 98927 7 None 58 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 297 5 0 4 2.8 CCOc1ccccc1N1CCN(Cc2cccnc2)CC1 10.1016/j.bmcl.2013.07.033
3303 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.9b01085
5311200 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.9b01085
CHEMBL267014 9024 46 None 1 15 Human 9.2 pKi = 9.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.9b01085
41532205 85052 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210717 85052 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
2653640 72993 12 None - 1 Human 9.2 pKi = 9.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 alleleIn vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 allele
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
CHEMBL184486 72993 12 None - 1 Human 9.2 pKi = 9.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 alleleIn vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4 allele
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
10450375 106267 0 None -1 4 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm981041x
CHEMBL28321 106267 0 None -1 4 Human 9.2 pKi = 9.2 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm981041x
41532205 85052 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1021/jm0611152
CHEMBL210717 85052 1 None 69 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1021/jm0611152
10643588 214202 0 None 239 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL94023 214202 0 None 239 3 Human 9.2 pKi = 9.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
71456045 90848 0 None 141 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207635 90848 0 None 141 6 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
49782398 24224 0 None 5 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 471 6 1 3 5.7 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL1257688 24224 0 None 5 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 471 6 1 3 5.7 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
122191607 130500 0 None 74 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622099 130500 0 None 74 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
25093832 162659 0 None -3 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 162659 0 None -3 5 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
1353 8692 93 None -3 85 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
3559 8692 93 None -3 85 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
86 8692 93 None -3 85 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
CHEMBL54 8692 93 None -3 85 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
DB00502 8692 93 None -3 85 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020952a
10594764 118550 0 None 19 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 0 4 4.0 Cc1c(-c2ccccc2)n(C)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL328739 118550 0 None 19 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 0 4 4.0 Cc1c(-c2ccccc2)n(C)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
4452 9538 19 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmcl.2021.128047
983 9538 19 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmcl.2021.128047
CHEMBL20734 9538 19 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmcl.2021.128047
CHEMBL5278853 200779 0 None 3311 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 316 3 1 3 3.4 N#Cc1[nH]c2ccccc2c1CN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2020.113141
44340097 16212 0 None 8 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL111749 16212 0 None 8 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
102505294 199778 0 None 309 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5204418 199778 0 None 309 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222691 199778 0 None 309 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
71454295 90854 0 None 30 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207641 90854 0 None 30 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
10638052 26864 0 None 70 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
CHEMBL130402 26864 0 None 70 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
60165418 82124 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.ejmech.2012.03.042
CHEMBL2037521 82124 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.ejmech.2012.03.042
10734727 26234 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL129757 26234 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
9977532 117968 1 None 6 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL326454 117968 1 None 6 4 Human 9.1 pKi = 9.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10783874 213826 0 None 13 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 0 4 3.7 Cn1c(-c2ccccc2)cn(C2CCN(Cc3ccccc3)CC2)c1=O 10.1021/jm991029k
CHEMBL91669 213826 0 None 13 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 0 4 3.7 Cn1c(-c2ccccc2)cn(C2CCN(Cc3ccccc3)CC2)c1=O 10.1021/jm991029k
10734727 26234 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
CHEMBL129757 26234 0 None 117 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 323 9 1 3 3.9 Fc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
60165418 82124 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL2037521 82124 0 None 8 6 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 353 6 0 6 3.2 c1cnc(N2CCN(CCCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
11697270 84085 0 None 44 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 412 5 0 5 4.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-c4ccccc4)c3n2)CC1 10.1021/jm060166w
CHEMBL208274 84085 0 None 44 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 412 5 0 5 4.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-c4ccccc4)c3n2)CC1 10.1021/jm060166w
10522614 213796 0 None 30 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.7 CCc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91498 213796 0 None 30 3 Human 9.1 pKi = 9.1 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 5 1 4 4.7 CCc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
4452 9538 19 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmc.2020.115578
983 9538 19 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmc.2020.115578
CHEMBL20734 9538 19 None -7 18 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1016/j.bmc.2020.115578
168274496 199591 0 None 724 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5175054 199591 0 None 724 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221490 199591 0 None 724 3 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 417 5 0 3 4.5 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
12765116 213298 1 None 6 3 Human 9.1 pKi = 9.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL88464 213298 1 None 6 3 Human 9.1 pKi = 9.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 326 1 0 3 4.2 CN1CCN(C2=Cc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
3303 9024 46 None 1 15 Human 9.0 pKi = 9.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm990277d
5311200 9024 46 None 1 15 Human 9.0 pKi = 9.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm990277d
CHEMBL267014 9024 46 None 1 15 Human 9.0 pKi = 9.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/jm990277d
3303 9024 46 None 1 15 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00252-2
5311200 9024 46 None 1 15 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00252-2
CHEMBL267014 9024 46 None 1 15 Human 9.0 pKi = 9.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00252-2
44400553 77554 0 None 3 5 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 77554 0 None 3 5 Human 9.0 pKi = 9.0 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
49788941 25046 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 5 1 5 1.6 N#Cc1cccnc1N1CCN(CCNC(=O)c2ccc(F)cc2)CC1 10.1021/jm100925m
CHEMBL1270423 25046 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 5 1 5 1.6 N#Cc1cccnc1N1CCN(CCNC(=O)c2ccc(F)cc2)CC1 10.1021/jm100925m
11689612 86614 0 None 436 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 388 5 0 7 2.9 COc1ccccc1N1CCN(Cc2cn3c(-n4cccn4)cccc3n2)CC1 10.1021/jm060166w
CHEMBL212160 86614 0 None 436 4 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 388 5 0 7 2.9 COc1ccccc1N1CCN(Cc2cn3c(-n4cccn4)cccc3n2)CC1 10.1021/jm060166w
10247720 19826 1 None 2 5 Human 9.0 pKi = 9.0 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 19826 1 None 2 5 Human 9.0 pKi = 9.0 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 19826 1 None 2 5 Human 9.0 pKi = 9.0 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; High binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
10447709 28058 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL131357 28058 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1016/j.bmcl.2005.02.012
76325150 113199 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 113199 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 113199 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
10248715 174656 0 None - 1 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 372 4 1 5 4.3 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(C#N)c2)CC1 10.1021/jm991029k
CHEMBL431095 174656 0 None - 1 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 372 4 1 5 4.3 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2cccc(C#N)c2)CC1 10.1021/jm991029k
10447709 28058 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1021/jm970422s
CHEMBL131357 28058 1 None 245 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 303 9 1 3 3.6 Cc1ccc(OCCNCCCOc2ccc(F)cc2)cc1 10.1021/jm970422s
76325150 113199 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 113199 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 113199 0 None 5 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
10236758 122550 5 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL3354065 122550 5 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
168268756 199543 0 None 1737 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5171439 199543 0 None 1737 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221187 199543 0 None 1737 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
10236758 122550 5 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354065 122550 5 None 208 13 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 328 7 0 2 4.3 CCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
11516033 145896 5 None 1023 6 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1016/j.ejmech.2019.111569
CHEMBL378680 145896 5 None 1023 6 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1016/j.ejmech.2019.111569
122180954 128547 0 None 1 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 368 7 1 3 4.5 CCCN(CCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589575 128547 0 None 1 3 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 368 7 1 3 4.5 CCCN(CCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
11575799 84904 0 None 1000 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 438 3 0 4 4.7 Clc1ccc(N2CCN(Cc3cn4cc(Br)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL210341 84904 0 None 1000 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 438 3 0 4 4.7 Clc1ccc(N2CCN(Cc3cn4cc(Br)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
11661609 86468 0 None 190 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 414 4 0 5 3.7 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(Br)c3n2)CC1 10.1021/jm060166w
CHEMBL211539 86468 0 None 190 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 414 4 0 5 3.7 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(Br)c3n2)CC1 10.1021/jm060166w
9951735 212034 0 None 8 3 Human 9.0 pKi = 9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 378 4 1 4 4.8 Nc1nc(-c2ccc(Cl)cc2)cc(C2CCN(Cc3ccccc3)CC2)n1 10.1021/jm970111h
CHEMBL78923 212034 0 None 8 3 Human 9.0 pKi = 9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 378 4 1 4 4.8 Nc1nc(-c2ccc(Cl)cc2)cc(C2CCN(Cc3ccccc3)CC2)n1 10.1021/jm970111h
10594242 213527 0 None 7 3 Human 9.0 pKi = 9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 5 4.5 Cc1c(-c2cccs2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL90005 213527 0 None 7 3 Human 9.0 pKi = 9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 5 4.5 Cc1c(-c2cccs2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
13014692 211700 1 None -1 4 Human 9.0 pKi = 9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3ccccc3Cc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL7617 211700 1 None -1 4 Human 9.0 pKi = 9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3ccccc3Cc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
1353 8692 93 None -3 85 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
3559 8692 93 None -3 85 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
86 8692 93 None -3 85 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
CHEMBL54 8692 93 None -3 85 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
DB00502 8692 93 None -3 85 Human 9.0 pKi = 9 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960268u
10314824 42154 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1016/j.ejmech.2020.113141
CHEMBL143761 42154 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1016/j.ejmech.2020.113141
10314824 42154 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL143761 42154 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
44412182 84041 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL208018 84041 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2006.02.075
10403608 84935 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210405 84935 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
44412182 84041 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1021/jm0611152
CHEMBL208018 84041 0 None 54 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1021/jm0611152
10403608 84935 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL210405 84935 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
10403608 84935 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL210405 84935 5 None 50 6 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
10314824 42154 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm060166w
CHEMBL143761 42154 1 None 8511 5 Human 9.0 pKi = 9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm060166w
1353 8692 93 None -3 85 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
3559 8692 93 None -3 85 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
86 8692 93 None -3 85 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
CHEMBL54 8692 93 None -3 85 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
DB00502 8692 93 None -3 85 Human 9.0 pKi = 9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991138z
102505294 199778 0 None 309 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5204418 199778 0 None 309 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222691 199778 0 None 309 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc(Cl)c2)CC1 10.1021/acs.jmedchem.2c00840
168289100 199730 0 None 316 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 374 5 0 4 3.1 N#Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5191299 199730 0 None 316 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 374 5 0 4 3.1 N#Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222419 199730 0 None 316 3 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 374 5 0 4 3.1 N#Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
10732925 121995 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL334545 121995 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1016/j.bmcl.2005.02.012
90644061 118810 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 118810 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
10666315 103364 0 None 47 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
CHEMBL263162 103364 0 None 47 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 361 4 1 4 4.7 Cc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
10809899 213524 0 None 34 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2Cl)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL89971 213524 0 None 34 3 Human 9.0 pKi = 9.0 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2Cl)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
511482 104027 6 None 53 5 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL268799 104027 6 None 53 5 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
10570479 119051 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL329106 119051 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 359 5 2 4 2.9 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
10732925 121995 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1021/jm970422s
CHEMBL334545 121995 1 None 269 3 Human 9.0 pKi = 9.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2ccccc2C)cc1 10.1021/jm970422s
10406796 106778 10 None -19 4 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL286725 106778 10 None -19 4 Human 9.0 pKi = 9.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
9805944 63001 37 None -1 9 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptorDisplacement of [3H]N-methylspiperone from dopamine D4 receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
CHEMBL1627 63001 37 None -1 9 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptorDisplacement of [3H]N-methylspiperone from dopamine D4 receptor
ChEMBL 462 7 2 3 4.7 CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1021/jm800510m
90644061 118810 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 118810 0 None 177 5 Rat 9.0 pKi = 9.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
9797495 75779 0 None 3548 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 328 3 0 4 2.9 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cc1 10.1021/jm200762g
CHEMBL1923292 75779 0 None 3548 5 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 328 3 0 4 2.9 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cc1 10.1021/jm200762g
44340227 117418 0 None 16 4 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325772 117418 0 None 16 4 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
10619737 209178 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
CHEMBL61079 209178 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
681 8247 72 None -2 38 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 8247 72 None -2 38 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 8247 72 None -2 38 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 8247 72 None -2 38 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 8247 72 None -2 38 Human 8.9 pKi = 8.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
10494394 175328 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1021/jm970422s
CHEMBL435598 175328 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1021/jm970422s
137651936 164171 0 None -1 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 164171 0 None -1 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
21219176 103066 0 None 12 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1nn(C2CCN(Cc3cccc(C#N)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL26120 103066 0 None 12 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1nn(C2CCN(Cc3cccc(C#N)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
10619737 209178 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm960072u
CHEMBL61079 209178 0 None 239 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 379 5 1 2 5.5 Cc1c(C2CCN(CCc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm960072u
45273045 203155 0 None 199 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL562620 203155 0 None 199 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
10427977 61239 0 None 660 4 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160952 61239 0 None 660 4 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
10494394 175328 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL435598 175328 1 None 158 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCNCCCOc2cccc(C)c2)cc1 10.1016/j.bmcl.2005.02.012
10088259 108690 3 None 134 3 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL300956 108690 3 None 134 3 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
10427977 61239 0 None 660 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
CHEMBL160952 61239 0 None 660 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
137640201 163740 2 None 177 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4072818 163740 2 None 177 13 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 362 6 0 2 4.3 O=C1CCc2ccccc2N1CCCN1CCC(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
9905249 106678 0 None 2 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL28607 106678 0 None 2 3 Human 8.9 pKi = 8.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
10762432 214192 0 None 46 3 Human 8.9 pKi = 8.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm991029k
CHEMBL93969 214192 0 None 46 3 Human 8.9 pKi = 8.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccc(Cl)cc2)CC1 10.1021/jm991029k
10740483 213910 0 None 20 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 413 7 2 4 3.5 C=CC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
CHEMBL92192 213910 0 None 20 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 413 7 2 4 3.5 C=CC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
44454709 104294 0 None 72 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 404 9 0 6 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
CHEMBL270406 104294 0 None 72 5 Human 8.9 pKi = 8.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 404 9 0 6 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
10450375 106267 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL28321 106267 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
16094698 144646 4 None 20 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
CHEMBL376092 144646 4 None 20 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 338 5 1 3 3.6 COc1ccccc1C1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm060662k
25256816 188387 0 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477206 188387 0 None -1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
10450375 106267 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL28321 106267 0 None -1 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 347 5 0 4 3.8 COc1ccccc1N1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
10406796 106778 10 None -19 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
CHEMBL286725 106778 10 None -19 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 369 7 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
25072002 162893 0 None -6 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 162893 0 None -6 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
11696910 84522 0 None 281 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 395 3 0 5 4.0 Clc1ccc2nc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cn2n1 10.1021/jm060166w
CHEMBL209034 84522 0 None 281 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 395 3 0 5 4.0 Clc1ccc2nc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cn2n1 10.1021/jm060166w
11631892 84886 0 None 2630 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 4 0 6 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1 10.1021/jm060166w
CHEMBL210283 84886 0 None 2630 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 4 0 6 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1 10.1021/jm060166w
10359942 109713 4 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc(CN2CC=C(c3nc4ccccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL306265 109713 4 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc(CN2CC=C(c3nc4ccccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
168294165 199791 0 None 204 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5209074 199791 0 None 204 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222773 199791 0 None 204 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1ccccc1N1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.2c00840
137645938 164362 0 None 204 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4080675 164362 0 None 204 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 342 8 0 2 4.6 CCCCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
9863333 211144 0 None 1 9 Rat 8.9 pKi = 8.9 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL71724 211144 0 None 1 9 Rat 8.9 pKi = 8.9 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
2470 10425 50 None -20 58 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
3300 10425 50 None -20 58 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
5265 10425 50 None -20 58 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
99 10425 50 None -20 58 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
CHEMBL267930 10425 50 None -20 58 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmc.2016.06.011
10615787 123541 0 None 67 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
CHEMBL337627 123541 0 None 67 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(OCCNCCCSc2ccccc2)cc1 10.1021/jm970422s
16094666 88502 3 None 52 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 88502 3 None 52 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
10498094 39092 1 None 1047 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4Cl)CC3)cc2c1 10.1021/jm0009989
CHEMBL141035 39092 1 None 1047 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4Cl)CC3)cc2c1 10.1021/jm0009989
122181333 128652 0 None 10 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590084 128652 0 None 10 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
11516033 145896 5 None 1023 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL378680 145896 5 None 1023 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1021/jm060166w
1353 8692 93 None -3 85 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
3559 8692 93 None -3 85 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
86 8692 93 None -3 85 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
CHEMBL54 8692 93 None -3 85 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
DB00502 8692 93 None -3 85 Human 8.9 pKi = 8.9 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
10314060 175379 0 None 72 6 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
CHEMBL435949 175379 0 None 72 6 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
1353 8692 93 None -3 85 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
3559 8692 93 None -3 85 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
86 8692 93 None -3 85 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
CHEMBL54 8692 93 None -3 85 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
DB00502 8692 93 None -3 85 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c00611
168285556 199696 0 None 2454 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196870 199696 0 None 2454 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222200 199696 0 None 2454 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting methodDisplacement of [3H]7-OH-DPAT from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1.5 hrs by MicroBeta scintillation counting method
ChEMBL 383 5 0 3 3.8 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.2c00840
9883587 118332 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 3 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL328054 118332 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 3 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
44394743 129879 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL361035 129879 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2004.07.045
10595908 212037 1 None 22 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.7 CCc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
CHEMBL78933 212037 1 None 22 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 5 1 2 5.7 CCc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
10567839 213812 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL91585 213812 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1016/j.ejmech.2020.113034
10716772 214065 0 None 20 2 Human 8.8 pKi = 8.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 415 7 2 4 3.7 CCC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
CHEMBL93198 214065 0 None 20 2 Human 8.8 pKi = 8.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 415 7 2 4 3.7 CCC(=O)Nc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1021/jm9601720
9883587 118332 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 321 3 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL328054 118332 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 321 3 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
12765746 109057 4 None -14 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL303313 109057 4 None -14 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
11725531 60828 2 None 1445 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/j.ejmech.2020.113141
CHEMBL160626 60828 2 None 1445 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/j.ejmech.2020.113141
CHEMBL5280364 200844 0 None 10000 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 381 5 1 4 3.8 CCOC(=O)c1[nH]c2ccc(F)cc2c1CN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2020.113141
11301655 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1016/j.ejmech.2020.113141
8441 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1016/j.ejmech.2020.113141
CHEMBL127257 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1016/j.ejmech.2020.113141
10473554 79722 0 None 2089 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 357 5 1 4 3.5 Clc1ccc(OCC2CN(Cc3c[nH]c4ncccc34)CCO2)cc1 10.1016/j.ejmech.2020.113141
CHEMBL2005767 79722 0 None 2089 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 357 5 1 4 3.5 Clc1ccc(OCC2CN(Cc3c[nH]c4ncccc34)CCO2)cc1 10.1016/j.ejmech.2020.113141
57403525 76929 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
57403525 76929 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940402 76929 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
CHEMBL1940402 76929 0 None 6 10 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
44394743 129879 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL361035 129879 0 None 39 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
25093832 162659 0 None -3 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 162659 0 None -3 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
137660837 165859 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 165859 0 None -2 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
71456046 90850 0 None 114 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207637 90850 0 None 114 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44381216 127110 0 None 8511 4 Human 8.8 pKi = 8.8 Binding
In vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cellsIn vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL352925 127110 0 None 8511 4 Human 8.8 pKi = 8.8 Binding
In vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cellsIn vitro ability to displace [3H]spiperone from the cloned human dopamine D4 receptor expressed in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
44371997 56704 0 None 10000 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 364 3 0 4 3.6 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)c(C)nn12 10.1016/s0960-894x(01)00814-9
CHEMBL156851 56704 0 None 10000 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 364 3 0 4 3.6 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)c(C)nn12 10.1016/s0960-894x(01)00814-9
11725531 60828 2 None 1445 5 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160626 60828 2 None 1445 5 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
11301655 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
8441 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
CHEMBL127257 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/jm030505a
11301655 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
8441 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL127257 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.7b00151
49788869 24996 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 365 6 1 6 1.5 COc1cccc(C(=O)NCCN2CCN(c3ncccc3C#N)CC2)c1 10.1021/jm100925m
CHEMBL1270121 24996 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 365 6 1 6 1.5 COc1cccc(C(=O)NCCN2CCN(c3ncccc3C#N)CC2)c1 10.1021/jm100925m
127049060 147553 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818478 147553 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
76321554 113180 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 113180 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 113180 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
9954003 78475 24 None -3 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
CHEMBL196514 78475 24 None -3 9 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 422 5 2 4 3.8 C[C@H]1Oc2c(cccc2N2CCN(CCCc3c[nH]c4ccc(F)cc34)CC2)NC1=O 10.1021/jm070516u
1353 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
3559 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
86 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
CHEMBL54 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
DB00502 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(01)00200-1
76321554 113180 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 113180 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 113180 0 None 5 5 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
44340084 15860 0 None 6 4 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL109912 15860 0 None 6 4 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10618875 110999 0 None 125 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.4 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
CHEMBL309901 110999 0 None 125 3 Human 8.8 pKi = 8.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.4 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccc(Cl)cc1 10.1021/jm970111h
9104271 210776 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL69584 210776 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(00)00421-2
44454711 104295 0 None 36 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2cccc(OCCF)c2)CC1 10.1016/j.bmcl.2007.12.026
CHEMBL270408 104295 0 None 36 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2cccc(OCCF)c2)CC1 10.1016/j.bmcl.2007.12.026
511482 104027 6 None 53 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
CHEMBL268799 104027 6 None 53 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
9104271 210776 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL69584 210776 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
9104271 210776 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)01056-9
CHEMBL69584 210776 12 None 436 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 369 4 0 3 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)01056-9
10336039 126013 1 None 15 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 318 4 0 4 3.2 c1ccc(-n2ccc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1021/jm00025a013
CHEMBL343466 126013 1 None 15 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 318 4 0 4 3.2 c1ccc(-n2ccc(CN3CCN(c4ccccn4)CC3)c2)cc1 10.1021/jm00025a013
127049060 147553 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818478 147553 0 None 13 7 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 402 6 2 3 3.9 O=C1NCN(c2ccccc2)C12CCN(CCCCc1c[nH]c3ccccc13)CC2 10.1016/j.bmc.2016.06.011
11682812 84984 0 None 239 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 402 5 0 7 3.2 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1 10.1021/jm060166w
CHEMBL210551 84984 0 None 239 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 402 5 0 7 3.2 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1 10.1021/jm060166w
11581237 145736 0 None 15 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 357 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cn3nc(Cl)ccc3n2)CC1 10.1021/jm060166w
CHEMBL378515 145736 0 None 15 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 357 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cn3nc(Cl)ccc3n2)CC1 10.1021/jm060166w
44376876 126950 0 None 27 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 322 4 0 3 3.7 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL351611 126950 0 None 27 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 322 4 0 3 3.7 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
155536720 178966 0 None 77 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 178966 0 None 77 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
10690200 213908 0 None 169 3 Human 8.8 pKi = 8.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 365 4 1 4 4.5 Cc1c(-c2ccc(F)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL92189 213908 0 None 169 3 Human 8.8 pKi = 8.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 365 4 1 4 4.5 Cc1c(-c2ccc(F)cc2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
44323978 112060 0 None 11 4 Human 8.8 pKi = 8.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 325 3 1 2 4.1 Clc1ccc2[nH]ccc2c1N1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(98)00474-0
CHEMBL311539 112060 0 None 11 4 Human 8.8 pKi = 8.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 325 3 1 2 4.1 Clc1ccc2[nH]ccc2c1N1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(98)00474-0
76316875 92662 0 None 18 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 321 3 1 0 3.4 Clc1ccc2[nH]ccc2c1-[n+]1cc[n+](Cc2ccccc2)cc1 10.1007/s00044-012-0055-5
CHEMBL2298810 92662 0 None 18 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 321 3 1 0 3.4 Clc1ccc2[nH]ccc2c1-[n+]1cc[n+](Cc2ccccc2)cc1 10.1007/s00044-012-0055-5
24882561 102116 0 None 58 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 408 8 0 5 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
CHEMBL256637 102116 0 None 58 5 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 408 8 0 5 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
155527714 178075 0 None 16 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 503 11 2 6 4.1 COc1ccc(N(Cc2ccccc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4460743 178075 0 None 16 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 503 11 2 6 4.1 COc1ccc(N(Cc2ccccc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
11726532 103801 0 None -2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
CHEMBL26677 103801 0 None -2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 368 8 0 5 3.5 COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
44376569 64215 0 None 19 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL165504 64215 0 None 19 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44376918 126790 0 None 109 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 323 4 0 4 3.1 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL350160 126790 0 None 109 2 Human 8.8 pKi = 8.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 323 4 0 4 3.1 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ccccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
42266988 25017 2 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 361 5 1 3 3.0 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100925m
CHEMBL1270227 25017 2 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 361 5 1 3 3.0 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100925m
168268695 199553 0 None 446 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5170580 199553 0 None 446 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5221253 199553 0 None 446 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 5 0 3 3.5 Cc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
21462964 54959 0 None 602 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL155207 54959 0 None 602 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
11792163 48850 0 None 316 2 Human 8.7 pKi = 8.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
CHEMBL149596 48850 0 None 316 2 Human 8.7 pKi = 8.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
44454735 102092 0 None 169 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 374 8 0 5 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
CHEMBL256492 102092 0 None 169 5 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 374 8 0 5 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
10643697 127901 1 None 10 3 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL357448 127901 1 None 10 3 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 383 8 1 5 2.6 COc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
44209472 76947 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940420 76947 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
44209472 76947 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940420 76947 2 None 1 11 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
2 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
54562 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
CHEMBL240773 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
2 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
54562 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
CHEMBL240773 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
2653640 72993 12 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
CHEMBL184486 72993 12 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccccc1N1CCN(CC(=O)Nc2cccc(C)c2)CC1 10.1016/j.bmcl.2004.07.068
2 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
54562 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
CHEMBL240773 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(03)00004-0
2 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
54562 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
CHEMBL240773 10035 23 None -2 28 Human 8.7 pKi = 8.7 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; high binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
4797946 177203 7 None 165 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 177203 7 None 165 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10837488 119429 0 None 6 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 6 2 4 3.9 COc1cc(NC(=O)C(F)(F)F)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL330318 119429 0 None 6 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 6 2 4 3.9 COc1cc(NC(=O)C(F)(F)F)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
22065971 127875 1 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1021/jm0002432
CHEMBL357182 127875 1 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1021/jm0002432
25256814 188391 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477250 188391 0 None 1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
71457844 90851 0 None 22 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207638 90851 0 None 22 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
1353 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
3559 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
86 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
CHEMBL54 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
DB00502 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2004.07.068
56652776 199787 0 None 257 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 319 5 0 3 3.9 c1ccc(N2CCN(CCCn3ccc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5205590 199787 0 None 257 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 319 5 0 3 3.9 c1ccc(N2CCN(CCCn3ccc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222747 199787 0 None 257 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 319 5 0 3 3.9 c1ccc(N2CCN(CCCn3ccc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
49788867 24978 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 380 6 1 6 2.4 COc1cccc(C(=O)NCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm100925m
CHEMBL1270013 24978 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 380 6 1 6 2.4 COc1cccc(C(=O)NCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm100925m
137642607 165297 0 None 234 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091231 165297 0 None 234 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 348 5 0 2 4.2 O=C1CCc2ccccc2N1CCCN1CCC(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
10588194 25692 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128524 25692 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
44336061 115398 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.8b00265
CHEMBL320597 115398 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.8b00265
135398737 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
38 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
722 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
CHEMBL42 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
DB00363 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970111h
10520941 211891 0 None 6 3 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 2 4.9 c1ccc(CCN2CCC(c3cc(C4CCCCC4)n[nH]3)CC2)cc1 10.1021/jm970111h
CHEMBL77744 211891 0 None 6 3 Human 8.0 pKi = 8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 2 4.9 c1ccc(CCN2CCC(c3cc(C4CCCCC4)n[nH]3)CC2)cc1 10.1021/jm970111h
9948584 214158 0 None -10 4 Human 8.0 pKi = 8 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL93779 214158 0 None -10 4 Human 8.0 pKi = 8 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
44273720 81970 0 None 100 2 Human 8.0 pKi = 8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 391 7 1 3 4.3 CC1(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
CHEMBL20367 81970 0 None 100 2 Human 8.0 pKi = 8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 391 7 1 3 4.3 CC1(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
9801098 12173 0 None 301 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 399 5 1 4 2.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CO 10.1016/s0960-894x(02)00656-x
CHEMBL107151 12173 0 None 301 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 399 5 1 4 2.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CO 10.1016/s0960-894x(02)00656-x
44335908 12761 0 None 21 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 425 5 0 3 4.6 CC(C)c1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL108011 12761 0 None 21 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 425 5 0 3 4.6 CC(C)c1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
135398737 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
38 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
722 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
CHEMBL42 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
DB00363 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9600712
135398737 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
38 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
722 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
CHEMBL42 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
DB00363 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960268u
44336075 11681 0 None 15 2 Human 8.0 pKi = 8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 378 5 0 3 4.3 COc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL104579 11681 0 None 15 2 Human 8.0 pKi = 8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 378 5 0 3 4.3 COc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
9948546 23096 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
CHEMBL122754 23096 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 6 2 4 3.3 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1 10.1021/jm990266k
44374827 126275 0 None 2 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 389 3 0 3 3.4 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL345438 126275 0 None 2 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 389 3 0 3 3.4 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL5277789 200727 0 None -7 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 405 8 2 5 3.7 Oc1cccc(OCCNCC2COCC(c3ccccc3)(c3ccccc3)O2)c1 10.1016/j.ejmech.2020.113141
164627977 193212 0 None -1 7 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4876297 193212 0 None -1 7 Human 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
1353 8692 93 None -4 85 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
3559 8692 93 None -4 85 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
86 8692 93 None -4 85 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
CHEMBL54 8692 93 None -4 85 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
DB00502 8692 93 None -4 85 Rat 8.0 pKi = 8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
52940985 24358 0 None 17 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1258155 24358 0 None 17 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
137651322 164254 0 None -11 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4079375 164254 0 None -11 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
135398737 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
135398737 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
38 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
38 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
722 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
722 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
CHEMBL42 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
CHEMBL42 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
DB00363 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00169-9
DB00363 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960072u
122180956 128549 0 None 8 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589577 128549 0 None 8 6 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
2389 10104 118 None -22 66 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
5073 10104 118 None -22 66 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
96 10104 118 None -22 66 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
CHEMBL85 10104 118 None -22 66 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
DB00734 10104 118 None -22 66 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm070516u
9887537 91120 43 None -12 9 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
CHEMBL221692 91120 43 None -12 9 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
CHEMBL4751170 91120 43 None -12 9 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 405 4 0 5 4.0 Fc1ccc(-c2cncc(CN3CCN(c4cccc5c4OCCO5)CC3)c2)cc1 10.1021/jm070516u
11725909 211047 0 None 33 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 357 3 1 2 5.2 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL71216 211047 0 None 33 3 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 357 3 1 2 5.2 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
1353 8692 93 None -3 85 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
3559 8692 93 None -3 85 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
86 8692 93 None -3 85 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
CHEMBL54 8692 93 None -3 85 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
DB00502 8692 93 None -3 85 Human 8.0 pKi = 8 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
9907461 141020 0 None - 1 Human 8.0 pKi = 8 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 371 4 1 3 3.8 O=C1NC(CCN2CCN(c3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
CHEMBL37169 141020 0 None - 1 Human 8.0 pKi = 8 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 371 4 1 3 3.8 O=C1NC(CCN2CCN(c3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
9903877 207105 1 None -6 5 Human 8.0 pKi = 8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 282 6 2 3 2.4 O=C1Cc2c(cccc2OCCNCc2ccccc2)N1 10.1016/s0960-894x(99)00434-5
CHEMBL59752 207105 1 None -6 5 Human 8.0 pKi = 8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 282 6 2 3 2.4 O=C1Cc2c(cccc2OCCNCc2ccccc2)N1 10.1016/s0960-894x(99)00434-5
135398737 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
38 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
722 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL42 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
DB00363 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/acs.jmedchem.7b00151
135398737 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
38 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
722 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
CHEMBL42 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
DB00363 7745 93 None -13 90 Human 8.0 pKi = 8 Binding
compound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell linescompound was tested for its affinity to displace [3H]spiperone cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991029k
127029388 146117 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792803 146117 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1cc(CN2CCO[C@H](COc3cccc(F)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
164938016 199748 0 None 67 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 337 5 0 4 4.1 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5200816 199748 0 None 67 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 337 5 0 4 4.1 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222506 199748 0 None 67 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 337 5 0 4 4.1 c1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1021/acs.jmedchem.2c00840
164627977 193212 0 None -1 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4876297 193212 0 None -1 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2cc(Cl)ccc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
127031516 146087 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792438 146087 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
92988697 146245 1 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794199 146245 1 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
1353 8692 93 None -3 85 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
3559 8692 93 None -3 85 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
86 8692 93 None -3 85 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
CHEMBL54 8692 93 None -3 85 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
DB00502 8692 93 None -3 85 Human 8.0 pKi = 8.0 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2003.07.015
9902382 49499 1 None 19 3 Human 8.0 pKi = 8.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL150173 49499 1 None 19 3 Human 8.0 pKi = 8.0 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
127029387 146185 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793612 146185 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 365 6 0 4 3.8 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
10590285 26826 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL130370 26826 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1016/j.bmcl.2005.02.012
12997400 107781 7 None 5 4 Human 7.0 pKi = 7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 241 3 1 2 2.3 c1ccc(N2CCN(Cc3ccc[nH]3)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL294394 107781 7 None 5 4 Human 7.0 pKi = 7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 241 3 1 2 2.3 c1ccc(N2CCN(Cc3ccc[nH]3)CC2)cc1 10.1016/s0960-894x(02)00316-5
11726130 63250 0 None 4 3 Human 7.0 pKi = 7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 361 1 0 1 6.3 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00004a016
CHEMBL163239 63250 0 None 4 3 Human 7.0 pKi = 7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 361 1 0 1 6.3 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00004a016
44273884 83833 0 None 2 2 Human 7.0 pKi = 7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20729 83833 0 None 2 2 Human 7.0 pKi = 7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2cccc(Cl)c2)CC1 10.1016/0960-894X(96)00198-9
9820048 210422 0 None 13 2 Human 7.0 pKi = 7 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 355 3 1 3 3.0 O=C1Nc2ccccc2CC1N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(00)00421-2
CHEMBL67222 210422 0 None 13 2 Human 7.0 pKi = 7 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 355 3 1 3 3.0 O=C1Nc2ccccc2CC1N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(00)00421-2
10811059 212393 5 None 23 3 Rat 7.0 pKi = 7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL81649 212393 5 None 23 3 Rat 7.0 pKi = 7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
135398737 7745 93 None -13 90 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 7745 93 None -13 90 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 7745 93 None -13 90 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 7745 93 None -13 90 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 7745 93 None -13 90 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398745 9688 112 None -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 9688 112 None -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 9688 112 None -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 9688 112 None -10 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
2389 10104 118 None -22 66 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 10104 118 None -22 66 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 10104 118 None -22 66 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 10104 118 None -22 66 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 10104 118 None -22 66 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
44403219 78679 0 None -91 5 Human 7.0 pKi = 7 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)nc1 10.1016/j.bmcl.2005.07.037
CHEMBL197162 78679 0 None -91 5 Human 7.0 pKi = 7 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)nc1 10.1016/j.bmcl.2005.07.037
242 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
72205043 98719 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 396 7 0 5 3.9 Clc1ccc(-n2cc(COCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414354 98719 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 396 7 0 5 3.9 Clc1ccc(-n2cc(COCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
118719927 122559 0 None 2 8 Human 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354074 122559 0 None 2 8 Human 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 386 11 1 3 4.4 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCCCO)CC1 10.1021/acs.jmedchem.8b00265
60165681 82131 0 None -3 6 Rat 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 7 0 5 5.1 O=C(CCCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037528 82131 0 None -3 6 Rat 7.0 pKi = 7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 7 0 5 5.1 O=C(CCCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
25139335 191097 0 None 2 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 10.1021/jm800895v
CHEMBL484203 191097 0 None 2 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 10.1021/jm800895v
57402366 76090 0 None -199 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928139 76090 0 None -199 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
72545239 99903 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443006 99903 0 None 1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
44436621 97806 0 None -17 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL239733 97806 0 None -17 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
242 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
34 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
60795 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
CHEMBL1112 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
DB01238 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm070516u
11245414 11891 0 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 362 6 1 5 3.2 COc1ccc(N)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105661 11891 0 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 362 6 1 5 3.2 COc1ccc(N)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
154703647 183144 1 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4450429 183144 1 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595728 183144 1 None -1 5 Human 7.0 pKi = 7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
242 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 7258 124 None -104 51 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
13014683 104118 0 None 1 2 Human 6.0 pKi = 6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.5 CC1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL269396 104118 0 None 1 2 Human 6.0 pKi = 6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.5 CC1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
1687 111186 20 None -275 5 Human 6.0 pKi = 6 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 341 4 0 2 5.1 CN1C2CCC1CC(OC(c1ccccc1)c1ccc(Cl)cc1)C2 10.1021/jm010146o
CHEMBL310310 111186 20 None -275 5 Human 6.0 pKi = 6 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 341 4 0 2 5.1 CN1C2CCC1CC(OC(c1ccccc1)c1ccc(Cl)cc1)C2 10.1021/jm010146o
CHEMBL540034 111186 20 None -275 5 Human 6.0 pKi = 6 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 341 4 0 2 5.1 CN1C2CCC1CC(OC(c1ccccc1)c1ccc(Cl)cc1)C2 10.1021/jm010146o
242 7258 124 None -104 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 7258 124 None -104 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 7258 124 None -104 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 7258 124 None -104 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 7258 124 None -104 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
33630 185736 99 None -13 28 Human 6.0 pKi = 6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 185736 99 None -13 28 Human 6.0 pKi = 6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
127046951 146680 0 None -21 6 Human 6.0 pKi = 6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799427 146680 0 None -21 6 Human 6.0 pKi = 6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
11360927 11743 0 None - 1 Human 6.0 pKi = 6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 377 7 0 5 3.6 COc1cccc(OCC2CN(Cc3ccc(Cl)cc3)CCO2)c1OC 10.1021/jm031111m
CHEMBL104844 11743 0 None - 1 Human 6.0 pKi = 6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 377 7 0 5 3.6 COc1cccc(OCC2CN(Cc3ccc(Cl)cc3)CCO2)c1OC 10.1021/jm031111m
145980271 173271 0 None -19 16 Human 5.0 pKi = 5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 173271 0 None -19 16 Human 5.0 pKi = 5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
46216855 207157 0 None -11220 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL597900 207157 0 None -11220 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231994 207187 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598105 207187 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231848 207317 0 None -3235 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598949 207317 0 None -3235 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231845 207512 0 None -3311 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL600083 207512 0 None -3311 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46232066 208035 0 None -14125 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
CHEMBL603872 208035 0 None -14125 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
11439190 208084 0 None -3548 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604127 208084 0 None -3548 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231995 208313 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605339 208313 0 None -16595 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231927 208315 0 None -10000 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605354 208315 0 None -10000 4 Human 5.0 pKi = 5 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
164627027 193206 0 None -50 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 466 5 3 4 4.3 O=C(NCc1ccccc1CN1CCc2cc(O)c(O)cc2C1)c1cccc(Br)c1 10.1016/j.bmcl.2021.128047
CHEMBL4876260 193206 0 None -50 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 466 5 3 4 4.3 O=C(NCc1ccccc1CN1CCc2cc(O)c(O)cc2C1)c1cccc(Br)c1 10.1016/j.bmcl.2021.128047
863787 73065 13 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
CHEMBL184772 73065 13 None - 1 Human 7.0 pKi = 7 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
168276065 196999 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5174753 196999 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.bmcl.2022.128615
168276065 196999 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL5174753 196999 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.ejmech.2022.114840
44395711 181678 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL456430 181678 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL537183 181678 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44395711 181678 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL456430 181678 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL537183 181678 0 None -5 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL5085974 221783 0 None -123 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
44309775 109455 0 None -288 7 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm049465g
CHEMBL304605 109455 0 None -288 7 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm049465g
44309775 109455 0 None -288 7 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
CHEMBL304605 109455 0 None -288 7 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
44309775 109455 0 None -288 7 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm040190e
CHEMBL304605 109455 0 None -288 7 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm040190e
72737772 121299 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335541 121299 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 295 5 0 2 3.8 Cc1ccccc1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
168276065 196999 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL5174753 196999 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 320 5 0 3 4.0 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(C#N)cc3)C2)cc1 10.1016/j.ejmech.2022.114840
56664948 73207 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 434 7 2 5 3.7 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5ccccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813587 73207 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 434 7 2 5 3.7 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5ccccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851962 73207 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 434 7 2 5 3.7 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5ccccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
44431482 94811 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234473 94811 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
1353 8692 93 None -3 85 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
3559 8692 93 None -3 85 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
86 8692 93 None -3 85 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
CHEMBL54 8692 93 None -3 85 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
DB00502 8692 93 None -3 85 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.ejmech.2006.12.030
10512444 31682 0 None -1445 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 1 2 2.2 CCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL134571 31682 0 None -1445 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 1 2 2.2 CCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
155536631 178999 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
CHEMBL4474014 178999 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
155536631 178999 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
CHEMBL4474014 178999 0 None -2 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 339 4 0 3 3.5 Fc1ccc2c(c1)CC(CCN1CCCN(c3ccccn3)CC1)C2 10.1016/j.bmc.2020.115943
42625295 63025 0 None -4073 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627321 63025 0 None -4073 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC(O)CCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
164612428 191942 0 None -14 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1ccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)cc1 10.1016/j.bmcl.2021.128047
CHEMBL4857166 191942 0 None -14 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1ccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)cc1 10.1016/j.bmcl.2021.128047
168296347 199241 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208643 199241 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 344 6 0 4 3.7 COc1ccc(CN2CCC[C@H](OCc3cccc(C)n3)C2)cc1F 10.1016/j.bmcl.2022.128615
154725484 183244 1 None -478 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4439544 183244 1 None -478 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596514 183244 1 None -478 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
168280974 197642 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5184607 197642 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
10983150 109765 0 None -13 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 7 0 4 4.6 O=C1c2ccccc2C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
CHEMBL306672 109765 0 None -13 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 7 0 4 4.6 O=C1c2ccccc2C(=O)N1CCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
763625 98923 7 None 19 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420775 98923 7 None 19 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
60165412 82134 0 None -28 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 7 0 5 4.5 O=C(CCCCN1CCN(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037530 82134 0 None -28 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 7 0 5 4.5 O=C(CCCCN1CCN(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
130431351 179950 0 None -3090 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 468 9 2 4 4.7 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4521947 179950 0 None -3090 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 468 9 2 4 4.7 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
168280974 197642 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5184607 197642 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
23288790 210743 0 None -123 6 Human 6.0 pKi = 6.0 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranesThe compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CCC3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
CHEMBL69385 210743 0 None -123 6 Human 6.0 pKi = 6.0 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranesThe compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CCC3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
9885219 63049 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL162873 63049 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
127031833 146173 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
CHEMBL3793347 146173 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1cccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c12 10.1016/j.bmcl.2016.03.102
135506137 18106 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 352 5 1 7 1.7 c1cnc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179504 18106 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 352 5 1 7 1.7 c1cnc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80655 18106 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 352 5 1 7 1.7 c1cnc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
10065188 108381 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL298763 108381 0 None 3 3 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
11408148 135498 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm049465g
CHEMBL366904 135498 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm049465g
11408148 135498 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL366904 135498 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
164623294 192602 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)c1 10.1016/j.bmcl.2021.128047
CHEMBL4867331 192602 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cccc(C(=O)NCc2ccccc2CN2CCc3cc(OC)c(O)cc3C2)c1 10.1016/j.bmcl.2021.128047
11408148 135498 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL366904 135498 0 None -275 5 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
72737725 121303 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
CHEMBL3335545 121303 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 317 5 0 2 3.8 Fc1cccc(F)c1CN1CCOC(CCc2ccccc2)C1 10.1021/ml500267c
4350931 176092 44 None -1348 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL441618 176092 44 None -1348 7 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
44336154 12212 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 4 0 3 4.2 CC1N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc2C1(C)C 10.1016/s0960-894x(02)00655-8
CHEMBL107384 12212 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 4 0 3 4.2 CC1N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc2C1(C)C 10.1016/s0960-894x(02)00655-8
4350931 176092 44 None -1348 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL441618 176092 44 None -1348 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
21302490 119582 32 None -12 9 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3233142 119582 32 None -12 9 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3306803 119582 32 None -12 9 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
188249 46427 4 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
CHEMBL147463 46427 4 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
CHEMBL2022280 46427 4 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm2013419
10363821 45811 0 None 91 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 403 2 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL146856 45811 0 None 91 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 403 2 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
10807035 213511 0 None 107 2 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 2 0 3 4.3 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
CHEMBL89921 213511 0 None 107 2 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 2 0 3 4.3 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
10615437 102716 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL25938 102716 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
15467370 109095 0 None 2818 4 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL303538 109095 0 None 2818 4 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
10807035 213511 0 None 107 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 339 2 0 3 4.3 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL89921 213511 0 None 107 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 339 2 0 3 4.3 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1016/j.ejmech.2020.113034
289 7030 12 None 1 14 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4.4 receptor by radioligand displacement assayBinding affinity to human D4.4 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
9948320 7030 12 None 1 14 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4.4 receptor by radioligand displacement assayBinding affinity to human D4.4 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
CHEMBL1242950 7030 12 None 1 14 Human 8.0 pKi = 8.0 Binding
Binding affinity to human D4.4 receptor by radioligand displacement assayBinding affinity to human D4.4 receptor by radioligand displacement assay
ChEMBL 301 8 0 2 4.9 CCCCC1CCN(CC1)CCCC(=O)c1ccccc1C 10.1021/jm100697g
72164301 98934 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 320 3 0 2 4.3 Clc1cccc(N2CCN(Cc3ccccc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420893 98934 0 None 3 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 320 3 0 2 4.3 Clc1cccc(N2CCN(Cc3ccccc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
44330553 174978 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 216 0 0 3 2.8 Cc1oc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL433376 174978 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 216 0 0 3 2.8 Cc1oc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
10590285 26826 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1021/jm970422s
CHEMBL130370 26826 1 None 21 3 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 299 9 1 3 3.7 Cc1ccc(OCCCNCCOc2ccc(C)cc2)cc1 10.1021/jm970422s
44335909 118116 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 6 0 4 3.8 CCOc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL326863 118116 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 6 0 4 3.8 CCOc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
10926404 53634 9 None 28 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 357 6 1 4 2.4 COc1cccc(C(=O)NCCN2CCN(c3ccc(F)cc3)CC2)c1 10.1021/jm020952a
CHEMBL154050 53634 9 None 28 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 357 6 1 4 2.4 COc1cccc(C(=O)NCCN2CCN(c3ccc(F)cc3)CC2)c1 10.1021/jm020952a
44335853 11631 0 None 478 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 3.8 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104321 11631 0 None 478 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 3.8 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
1353 8692 93 None -3 85 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
3559 8692 93 None -3 85 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
86 8692 93 None -3 85 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
CHEMBL54 8692 93 None -3 85 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
DB00502 8692 93 None -3 85 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
10782946 22345 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL122049 22345 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)cc1 10.1021/jm990266k
9906978 49485 2 None 1 12 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL150161 49485 2 None 1 12 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
2435 10362 83 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
60149 10362 83 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
98 10362 83 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
CHEMBL12713 10362 83 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
DB06144 10362 83 None -10 48 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
145969934 171824 0 None 1 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4226336 171824 0 None 1 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
11504230 84992 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm100899z
CHEMBL210567 84992 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm100899z
11393666 199765 0 None -28 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 199765 0 None -28 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 199765 0 None -28 19 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL4435399 220703 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None O=[N+]([O-])c1ccc(CN2CCC(n3cc(Cc4ccc(Br)cc4)nn3)CC2)cc1 10.1016/j.bmc.2022.116851
16725912 92504 15 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
16725912 92504 15 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL228972 92504 15 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL228972 92504 15 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
44431489 95046 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL234825 95046 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
53364155 70618 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 33 0 16 10.2 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCCc1cn(CCCCCCCCCCn2cc(CCCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803026 70618 0 None 1 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 33 0 16 10.2 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCCc1cn(CCCCCCCCCCn2cc(CCCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
137632761 163353 0 None -13 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
CHEMBL4068561 163353 0 None -13 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
137640203 163741 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
CHEMBL4072821 163741 0 None -1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
10615437 102716 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL25938 102716 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
71733935 97758 0 None -43 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
CHEMBL2396663 97758 0 None -43 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
10615437 102716 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cellsDisplacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/j.bmc.2022.116851
CHEMBL25938 102716 1 None 6 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cellsDisplacement of [3H]spiperone from recombinant human D4 receptor stably expressed in HEK293 cells
ChEMBL 317 4 1 2 4.5 c1ccc(CN2CCC(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1016/j.bmc.2022.116851
9865446 130829 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CCC(O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
CHEMBL36313 130829 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CCC(O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
10479188 209652 0 None 5 4 Human 8.0 pKi = 8.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL62602 209652 0 None 5 4 Human 8.0 pKi = 8.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
9949531 213388 0 None -11 4 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 333 6 3 4 3.7 Sc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL89037 213388 0 None -11 4 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 333 6 3 4 3.7 Sc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
44369020 126237 0 None -2 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm100925m
CHEMBL345111 126237 0 None -2 3 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm100925m
11558055 79927 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL1204122 79927 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL201170 79927 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
11558055 79927 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL1204122 79927 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL201170 79927 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
11558055 79927 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL1204122 79927 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 79927 1 None -17 6 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
11772112 175595 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
CHEMBL437687 175595 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1C 10.1021/jm060279f
44278427 106118 0 None 39 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL282323 106118 0 None 39 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
127031518 146177 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793389 146177 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
127029995 146275 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3794529 146275 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1F 10.1016/j.bmcl.2016.03.102
11849266 87844 0 None 5 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
CHEMBL215450 87844 0 None 5 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.6 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(C)c1 10.1021/jm060279f
44370047 126454 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 340 4 1 3 3.5 Clc1ccc(N2CCN(CCc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL347155 126454 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 340 4 1 3 3.5 Clc1ccc(N2CCN(CCc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
13091268 84999 0 None -8 14 Human 7.9 pKi = 7.9 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
CHEMBL210578 84999 0 None -8 14 Human 7.9 pKi = 7.9 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
10378389 210024 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 210024 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 210024 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
10378389 210024 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 210024 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 210024 1 None -53 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
10497193 211716 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 4 1 2 4.7 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL76355 211716 0 None 1 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 4 1 2 4.7 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
10738530 211814 0 None 5 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 6 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CCCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL77017 211814 0 None 5 3 Human 7.0 pKi = 7.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 379 6 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CCCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
10790517 214391 0 None 10 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 469 7 2 4 4.9 COc1cc(NC(=O)C2CCCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL95096 214391 0 None 10 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 469 7 2 4 4.9 COc1cc(NC(=O)C2CCCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
6603867 108771 17 None -56 7 Human 7.0 pKi = 7.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL301559 108771 17 None -56 7 Human 7.0 pKi = 7.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2ccc(O)cc2C1 10.1021/jm960345l
57345618 77234 0 None -1 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 362 6 0 3 4.5 Fc1ccc(OCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946126 77234 0 None -1 6 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 362 6 0 3 4.5 Fc1ccc(OCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
92984956 146258 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794363 146258 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccc(OC)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
11164276 86527 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL211732 86527 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
11154555 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
5037 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
7671 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL2028019 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL3085826 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB06016 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
11154555 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
5037 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
7671 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL2028019 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL3085826 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
DB06016 7587 62 None -501 12 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
10830557 38075 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(F)cc4)CC3)c2c1 10.1021/jm0009989
CHEMBL140165 38075 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(F)cc4)CC3)c2c1 10.1021/jm0009989
44436600 98577 0 None -109 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241212 98577 0 None -109 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
71734126 97829 0 None -10 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
CHEMBL2397391 97829 0 None -10 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
44372312 60559 0 None 43 3 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
CHEMBL160396 60559 0 None 43 3 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
72737734 121300 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
CHEMBL3335542 121300 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1cccc(CN2CCOC(CCc3ccccc3)C2)c1 10.1021/ml500267c
155536815 178986 0 None 33 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
CHEMBL4473792 178986 0 None 33 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 322 4 1 2 4.1 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1021/acs.jmedchem.9b00231
133633 9021 53 None -104 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
177 9021 53 None -104 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
CHEMBL445102 9021 53 None -104 8 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
44438201 100382 2 None -158 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246637 100382 2 None -158 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
25139329 193882 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
CHEMBL491466 193882 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
2779264 118119 38 None 8 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 240 3 0 2 3.3 c1ccc(CN2CCC(n3cccc3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL326877 118119 38 None 8 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 240 3 0 2 3.3 c1ccc(CN2CCC(n3cccc3)CC2)cc1 10.1016/s0960-894x(99)00540-5
134151428 161331 0 None -44 9 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 3 0 2 3.5 O=C1c2ccccc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3978642 161331 0 None -44 9 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 3 0 2 3.5 O=C1c2ccccc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991094 161331 0 None -44 9 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 3 0 2 3.5 O=C1c2ccccc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
17755999 149663 1 None -190 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
CHEMBL389357 149663 1 None -190 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
3117 214620 103 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 214620 103 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
44304644 210030 0 None 1 4 Human 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 454 8 2 4 4.5 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)c[nH]1 10.1016/s0960-894x(00)00405-4
CHEMBL64566 210030 0 None 1 4 Human 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 454 8 2 4 4.5 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)c[nH]1 10.1016/s0960-894x(00)00405-4
10436285 108729 0 None -478 4 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
CHEMBL301242 108729 0 None -478 4 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
10301202 20274 0 None -70 3 Human 6.0 pKi = 6.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1193508 20274 0 None -70 3 Human 6.0 pKi = 6.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL544925 20274 0 None -70 3 Human 6.0 pKi = 6.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
11211058 87109 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL214247 87109 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(\c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
44393737 72535 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
CHEMBL183466 72535 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
154703824 183405 1 None -436 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4456007 183405 1 None -436 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597876 183405 1 None -436 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
145967904 171876 0 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4227192 171876 0 None 1 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
11812838 210664 0 None -47 4 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.4 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
CHEMBL68860 210664 0 None -47 4 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.4 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
154726046 183090 1 None -288 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4442408 183090 1 None -288 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595266 183090 1 None -288 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
168282745 197874 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5187721 197874 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
168288343 198236 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5193214 198236 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.ejmech.2022.114840
136094867 47343 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 443 3 2 5 5.7 Clc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148353 47343 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 443 3 2 5 5.7 Clc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
155511803 176384 0 None 229 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4436479 176384 0 None 229 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 342 4 1 2 4.5 Cc1cccc(NC(=O)CN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/acs.jmedchem.9b00231
164622586 192315 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 470 6 2 4 5.2 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4862839 192315 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 470 6 2 4 5.2 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2021.128047
168288343 198236 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5193214 198236 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.ejmech.2022.114840
168288343 198236 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5193214 198236 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 440 6 1 3 5.3 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2022.128615
168282745 197874 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5187721 197874 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
10378389 210024 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(01)00778-8
CHEMBL134807 210024 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(01)00778-8
CHEMBL64553 210024 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(01)00778-8
10378389 210024 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL134807 210024 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL64553 210024 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm9703653
10378389 210024 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(98)00014-6
CHEMBL134807 210024 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(98)00014-6
CHEMBL64553 210024 1 None -53 7 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1016/s0960-894x(98)00014-6
44431462 94844 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234640 94844 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
10411988 28182 0 None -29 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL131482 28182 0 None -29 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 461 6 0 5 5.2 CC1SC2(CCCC2)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
122334 7110 23 None -2 7 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
970 7110 23 None -2 7 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
CHEMBL27441 7110 23 None -2 7 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
122334 7110 23 None -2 7 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1021/jm00073a021
970 7110 23 None -2 7 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1021/jm00073a021
CHEMBL27441 7110 23 None -2 7 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1021/jm00073a021
22727358 19996 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 367 7 0 5 4.5 c1ccc(N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1191251 19996 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 367 7 0 5 4.5 c1ccc(N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL542324 19996 0 None -7 3 Human 6.9 pKi = 6.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 367 7 0 5 4.5 c1ccc(N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
127049059 147591 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818935 147591 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
85658088 171782 0 None -3 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225830 171782 0 None -3 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
127049059 147591 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818935 147591 0 None -11 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 404 6 1 5 3.6 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3o1)CC2 10.1016/j.bmc.2016.06.011
72205222 98723 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 408 8 0 4 5.1 Clc1ccc(-n2cc(CCCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414358 98723 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 408 8 0 4 5.1 Clc1ccc(-n2cc(CCCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
162669562 189481 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4789472 189481 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
44431467 161211 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL398990 161211 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2cccc(C(F)(F)F)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
44438229 161678 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 380 6 1 2 5.5 C=CCOC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL400826 161678 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 380 6 1 2 5.5 C=CCOC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
142590728 188301 0 None -3 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 446 7 1 3 5.4 CC(C)(C)C(=O)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4765081 188301 0 None -3 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 446 7 1 3 5.4 CC(C)(C)C(=O)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
10618211 85378 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 355 5 1 3 4.7 O=C(/C=C(\O)c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1021/jm970111h
CHEMBL2112285 85378 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 355 5 1 3 4.7 O=C(/C=C(\O)c1ccc(Cl)cc1)C1CCN(Cc2ccccc2)CC1 10.1021/jm970111h
44300865 208774 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL60815 208774 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
10424172 20560 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 287 1 0 1 4.4 CN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1195497 20560 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 287 1 0 1 4.4 CN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL554670 20560 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 287 1 0 1 4.4 CN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
44323894 174879 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL432762 174879 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
10619612 179459 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
CHEMBL450021 179459 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 377 5 1 5 4.4 COc1ccc(-c2nc(O)n(C3CCN(Cc4ccccc4)CC3)c2C)cc1 10.1021/jm991029k
44323894 174879 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL432762 174879 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10617381 196465 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
CHEMBL51536 196465 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1021/jm970021c
44454710 162445 0 None 70 5 Human 7.9 pKi = 7.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 378 7 0 4 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
CHEMBL404888 162445 0 None 70 5 Human 7.9 pKi = 7.9 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 378 7 0 4 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
9859861 174859 1 None 173 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL432579 174859 1 None 173 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 1 2 3.2 Cc1sc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
44335973 11806 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)ccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105172 11806 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)ccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
44335893 115382 0 None 16 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)c(F)c2Cl)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL320515 115382 0 None 16 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)c(F)c2Cl)CC1 10.1016/s0960-894x(02)00656-x
44335746 12471 0 None 251 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 3 3.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)cc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107804 12471 0 None 251 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 3 3.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)cc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
44335829 115373 0 None 147 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 391 5 0 3 3.9 CC(C)c1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL320440 115373 0 None 147 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 391 5 0 3 3.9 CC(C)c1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44335828 170236 0 None 158 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(C)(C)C)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL419916 170236 0 None 158 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(C)(C)C)cc2)CC1 10.1016/s0960-894x(02)00655-8
155561779 182544 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 566 10 2 6 5.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4583596 182544 0 None 9 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 566 10 2 6 5.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
44374863 126985 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 403 3 0 3 3.8 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL351989 126985 0 None 13 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 403 3 0 3 3.8 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(C3=O)C(C)(C)C5)CC2)cc1 10.1016/s0960-894x(02)01056-9
90644057 118809 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289645 118809 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
13091268 84999 0 None -13 14 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL210578 84999 0 None -13 14 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
53364226 70620 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 989 29 0 18 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803028 70620 0 None -3 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 989 29 0 18 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53363201 70629 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 893 27 0 15 7.0 COc1cc(CN2CCN(C)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803054 70629 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 893 27 0 15 7.0 COc1cc(CN2CCN(C)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
44300865 208774 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL60815 208774 0 None 16 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/j.bmcl.2006.02.075
44436599 98576 0 None 5 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
CHEMBL241211 98576 0 None 5 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
44222483 203030 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL561763 203030 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
45271653 202014 0 None 851 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)ncn34)CC2)cc1 10.1016/j.bmc.2009.05.015
CHEMBL550920 202014 0 None 851 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)ncn34)CC2)cc1 10.1016/j.bmc.2009.05.015
10251080 20731 0 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 411 9 0 6 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1196692 20731 0 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 411 9 0 6 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL557829 20731 0 None -3 3 Human 7.9 pKi = 7.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 411 9 0 6 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
13091268 84999 0 None -8 14 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
CHEMBL210578 84999 0 None -8 14 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2003.07.015
10617381 196465 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL51536 196465 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
11792373 126600 0 None 457 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL348435 126600 0 None 457 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
127053214 146127 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3792923 146127 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 311 5 0 3 3.6 Cc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
76282192 199812 0 None 724 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 0 4 3.2 c1ccc(N2CCN(CCCn3cnc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5207313 199812 0 None 724 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 0 4 3.2 c1ccc(N2CCN(CCCn3cnc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222877 199812 0 None 724 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 0 4 3.2 c1ccc(N2CCN(CCCn3cnc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
9949601 106829 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 335 4 1 3 3.0 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL287078 106829 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 335 4 1 3 3.0 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
44264644 211522 0 None 87 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 330 3 0 4 3.2 Clc1ccc(N2CCN(Cc3cnn4c3CCCC4)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7442 211522 0 None 87 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 330 3 0 4 3.2 Clc1ccc(N2CCN(Cc3cnn4c3CCCC4)CC2)cc1 10.1016/s0960-894x(98)00692-1
155563301 182029 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 182029 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
44273927 82320 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 379 9 1 3 4.2 CCCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20444 82320 0 None 125 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 379 9 1 3 4.2 CCCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44273924 82682 0 None 199 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20493 82682 0 None 199 2 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
9863108 84851 0 None -12 3 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21008 84851 0 None -12 3 Human 7.9 pKi = 7.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
90644057 118809 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289645 118809 0 None 28 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
1353 8692 93 None -3 85 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
3559 8692 93 None -3 85 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
86 8692 93 None -3 85 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
CHEMBL54 8692 93 None -3 85 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
DB00502 8692 93 None -3 85 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.12.054
10382581 108075 0 None 151 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL296506 108075 0 None 151 3 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
90644067 118797 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289383 118797 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
11724853 103795 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 340 0 0 4 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C)c3ccccc32)CC1 10.1021/jm00043a008
CHEMBL266723 103795 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 340 0 0 4 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C)c3ccccc32)CC1 10.1021/jm00043a008
12066264 21187 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 469 6 0 2 7.4 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cccc3ccccc23)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL12004 21187 0 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 469 6 0 2 7.4 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cccc3ccccc23)c2ccc(F)cc2)cc1 10.1021/jm010146o
11849182 86644 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL212288 86644 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 417 9 1 7 2.7 CO/N=C(/c1ccc(Cl)cc1)C(CNOC)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
49782836 24324 0 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 456 6 0 3 5.5 O=C(CCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL1258036 24324 0 None -12 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 456 6 0 3 5.5 O=C(CCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
49782837 24357 0 None 3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 472 6 0 3 6.0 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1258154 24357 0 None 3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 472 6 0 3 6.0 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
11706497 84952 0 None -33 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL210461 84952 0 None -33 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
44436605 155842 0 None -389 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL394292 155842 0 None -389 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
11517928 83878 0 None 7 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 444 4 0 6 4.3 Clc1ccc(N2CCN(Cc3cn4nc(N5CCCCC5)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL207543 83878 0 None 7 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 444 4 0 6 4.3 Clc1ccc(N2CCN(Cc3cn4nc(N5CCCCC5)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
45269161 203114 0 None 5 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 336 3 0 6 2.4 Cc1cc2nc(C)c(CN3CCN(c4ccccn4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL562384 203114 0 None 5 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 336 3 0 6 2.4 Cc1cc2nc(C)c(CN3CCN(c4ccccn4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
44381424 65845 0 None 53 4 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL169562 65845 0 None 53 4 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
162669562 189481 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4789472 189481 0 None -2 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 0 4 4.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cn1)C2)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
168270809 196827 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.ejmech.2022.114840
CHEMBL5172055 196827 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.ejmech.2022.114840
164623862 192784 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
CHEMBL4870361 192784 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
168270809 196827 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5172055 196827 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.bmcl.2022.128615
10826290 212262 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 275 2 1 2 3.5 CN1CCC(c2cc(-c3ccc(Cl)cc3)[nH]n2)CC1 10.1021/jm970111h
CHEMBL80552 212262 0 None - 1 Human 5.9 pKi = 5.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 275 2 1 2 3.5 CN1CCC(c2cc(-c3ccc(Cl)cc3)[nH]n2)CC1 10.1021/jm970111h
21219173 100230 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnnc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL24603 100230 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnnc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
44319361 212499 0 None -1 4 Human 5.9 pKi = 5.9 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL82527 212499 0 None -1 4 Human 5.9 pKi = 5.9 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
71717830 92758 0 None 9 2 Human 5.9 pKi = 5.9 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
CHEMBL2303762 92758 0 None 9 2 Human 5.9 pKi = 5.9 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@H](Oc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@H](O)[C@H]1O 10.1016/S0960-894X(97)00194-7
168280776 197937 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5188602 197937 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
44374637 62039 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 393 7 0 4 4.5 CCCN(CCC)[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL161811 62039 0 None -3 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 393 7 0 4 4.5 CCCN(CCC)[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
168270809 196827 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.ejmech.2022.114840
CHEMBL5172055 196827 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 392 6 1 3 4.0 Cc1cc(NC(=O)CN2CCC(OCc3ccc(F)c(F)c3)CC2)ccc1F 10.1016/j.ejmech.2022.114840
164623862 192784 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
CHEMBL4870361 192784 0 None -6 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 351 6 0 5 2.8 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc21 10.1016/j.ejmech.2021.113243
168280776 197937 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5188602 197937 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
44591089 196261 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 10.1016/j.bmc.2008.12.054
CHEMBL513776 196261 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 10.1016/j.bmc.2008.12.054
57390695 77242 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946257 77242 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
57390695 77242 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL1946257 77242 0 None -9 8 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 427 7 0 5 5.5 O=C(CCCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
127052778 147623 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819403 147623 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
164623991 192316 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 192316 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
9980998 37808 0 None -524 7 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL139926 37808 0 None -524 7 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL2112911 37808 0 None -524 7 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
11203294 82606 3 None -190 5 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
CHEMBL2048623 82606 3 None -190 5 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
3695490 107371 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 355 8 1 4 3.4 COc1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL29179 107371 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 355 8 1 4 3.4 COc1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
57345619 77239 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 360 6 0 2 5.0 Fc1ccc(CCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946253 77239 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 360 6 0 2 5.0 Fc1ccc(CCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
127050699 147650 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819082 147650 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819726 147650 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 3 0 1 4.0 Fc1ccc2c(c1)CC(CCN1CCc3ccccc3C1)C2 10.1016/j.bmc.2016.05.053
164623991 192316 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4862890 192316 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 410 10 2 4 4.2 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
25141533 98942 0 None -676 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 471 8 2 5 3.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
CHEMBL242218 98942 0 None -676 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 471 8 2 5 3.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
9888494 104947 0 None -549 13 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human dopamine D4 receptor was determinedBinding affinity towards cloned human dopamine D4 receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
CHEMBL273921 104947 0 None -549 13 Human 5.9 pKi = 5.9 Binding
Binding affinity towards cloned human dopamine D4 receptor was determinedBinding affinity towards cloned human dopamine D4 receptor was determined
ChEMBL 422 4 1 5 3.6 O=C1c2ccccc2CCCN1CCN1CCC(n2c(O)nc3cc(F)ccc32)CC1 10.1016/s0960-894x(03)00077-5
73213196 111237 4 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 111237 4 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
127052778 147623 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819403 147623 0 None -7 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 505 9 0 5 6.3 O=C(CCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
11203294 82606 3 None -190 5 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
CHEMBL2048623 82606 3 None -190 5 Human 5.9 pKi = 5.9 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL 526 9 1 5 5.7 Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 10.6019/CHEMBL5058642
CHEMBL5086258 221798 0 None -199 6 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor by radioligand binding assayBinding affinity to human D4 receptor by radioligand binding assay
ChEMBL None None None Cc1cc(I)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
136094687 20210 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 429 7 1 6 4.2 c1ccc2c(c1)N=C(NCCCCCN1CCN(c3ccc4ccccc4n3)CC1)CO2 10.1016/S0960-894X(97)00442-3
CHEMBL1192972 20210 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 429 7 1 6 4.2 c1ccc2c(c1)N=C(NCCCCCN1CCN(c3ccc4ccccc4n3)CC1)CO2 10.1016/S0960-894X(97)00442-3
CHEMBL544296 20210 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 429 7 1 6 4.2 c1ccc2c(c1)N=C(NCCCCCN1CCN(c3ccc4ccccc4n3)CC1)CO2 10.1016/S0960-894X(97)00442-3
15467373 108631 0 None 60 4 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(99)00302-9
CHEMBL300553 108631 0 None 60 4 Human 6.9 pKi = 6.9 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(99)00302-9
44273715 79898 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 7 1 3 3.0 CC(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20114 79898 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 7 1 3 3.0 CC(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44273877 105510 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 335 6 1 3 2.9 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL277937 105510 0 None 15 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 335 6 1 3 2.9 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(F)cc2)CC1 10.1016/0960-894X(96)00198-9
44273553 105564 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 7 1 3 3.8 CC(C)(C)C(=O)NCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL278288 105564 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 7 1 3 3.8 CC(C)(C)C(=O)NCCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
134155461 161266 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3959209 161266 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3990475 161266 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
44273552 86705 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 309 6 1 3 2.4 CC(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21252 86705 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 309 6 1 3 2.4 CC(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
9827938 18543 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181680 18543 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188486 18543 0 None -50 12 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
57402951 77243 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946258 77243 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
57402951 77243 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL1946258 77243 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 413 6 0 5 5.1 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL5071238 221032 0 None -10 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CC(O)CCNCCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
CHEMBL5070377 221014 0 None -251 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
11335419 73874 1 None -125 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL187367 73874 1 None -125 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
134155461 161266 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3959209 161266 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3990475 161266 0 None -1 6 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 291 4 1 2 3.6 c1ccc2c(c1)CCN(CCCc1nc3ccccc3[nH]1)C2 10.1016/j.bmc.2016.09.019
44376921 64099 0 None 2 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 382 5 0 7 2.2 COC(=O)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL165113 64099 0 None 2 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 382 5 0 7 2.2 COC(=O)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
49783415 24450 0 None -1698 12 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
CHEMBL1258452 24450 0 None -1698 12 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 320 7 1 5 2.9 CCCCN1CCC(COC(=O)c2ccc(N)c(OC)c2)CC1 10.1021/jm100668r
134133968 161302 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3899099 161302 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3990801 161302 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
10476504 40261 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL142020 40261 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
11663604 89948 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 520 13 1 8 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccc(OC)cc1 10.1021/jm0611152
CHEMBL218351 89948 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 520 13 1 8 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccc(OC)cc1 10.1021/jm0611152
155539605 179624 0 None -5 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
CHEMBL4514672 179624 0 None -5 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 receptor by radioligand binding assay
ChEMBL 313 1 0 4 2.1 CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O 10.1016/j.ejmech.2018.12.048
46912548 21165 0 None -144 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1173288 21165 0 None -144 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1200271 21165 0 None -144 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
44438210 100146 2 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 2 2 5.3 OC1(c2ccc(-c3ccccc3)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL245615 100146 2 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 2 2 5.3 OC1(c2ccc(-c3ccccc3)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
134133968 161302 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3899099 161302 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3990801 161302 0 None -4 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1cccc2c1CN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.09.019
42625293 63023 0 None -316 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL1627319 63023 0 None -316 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
44330292 11280 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1ncn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL102162 11280 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1ncn(C)c1-2 10.1016/s0960-894x(03)00587-0
44330515 215177 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 0 1 2 3.9 Cc1sc(C)c2c1CC(C)(C)Cc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL99654 215177 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 0 1 2 3.9 Cc1sc(C)c2c1CC(C)(C)Cc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
154706711 183294 1 None -47 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4439535 183294 1 None -47 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4596930 183294 1 None -47 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
10760813 170868 5 None 9 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CC4CCCCC4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL420954 170868 5 None 9 3 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 5.5 Clc1ccc(-c2cc(C3CCN(CC4CCCCC4)CC3)[nH]n2)cc1 10.1021/jm970111h
44264623 211792 0 None 407 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnc4ccccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7686 211792 0 None 407 4 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnc4ccccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44336138 11645 0 None 75 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 419 6 0 4 3.2 O=S1(=O)Cc2ccccc2N1CCCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104380 11645 0 None 75 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 419 6 0 4 3.2 O=S1(=O)Cc2ccccc2N1CCCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
90644067 118797 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289383 118797 0 None 48 3 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 380 6 0 3 3.8 [O-][S+](CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
90644060 118808 0 None 64 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 358 4 0 2 4.4 Fc1ccc2c(c1)CC(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmc.2014.04.026
CHEMBL3289644 118808 0 None 64 4 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 358 4 0 2 4.4 Fc1ccc2c(c1)CC(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmc.2014.04.026
135398737 7745 93 None -13 90 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
38 7745 93 None -13 90 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
722 7745 93 None -13 90 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
CHEMBL42 7745 93 None -13 90 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
DB00363 7745 93 None -13 90 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00218-7
53363110 70625 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 507 14 0 8 4.8 CCCCn1cc(CCCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803050 70625 0 None 4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 507 14 0 8 4.8 CCCCn1cc(CCCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
24936042 164368 0 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 164368 0 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
6603820 102549 19 None -1 12 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
CHEMBL25856 102549 19 None -1 12 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from rat dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
11428416 12067 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 361 7 0 4 4.0 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL106599 12067 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 361 7 0 4 4.0 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11406804 171241 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL421403 171241 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
127029386 146175 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793375 146175 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccc(F)cc3)C2)cc1 10.1016/j.bmcl.2016.03.102
11772767 86777 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
CHEMBL212784 86777 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(Cl)c1 10.1021/jm060279f
164628817 193056 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
CHEMBL4874069 193056 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
11849775 172975 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL426510 172975 0 None 7 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
44340376 117423 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325818 117423 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10476504 40261 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL142020 40261 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
44403214 79268 0 None -9 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)nc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL198993 79268 0 None -9 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)nc2)CC1 10.1016/j.bmcl.2005.07.037
44393393 130451 0 None -91 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 537 7 1 4 5.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)s1 10.1016/j.bmcl.2004.05.052
CHEMBL362101 130451 0 None -91 5 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 537 7 1 4 5.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)s1 10.1016/j.bmcl.2004.05.052
44381147 65503 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168544 65503 0 None -3 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
55445 105324 18 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 219 3 1 2 3.0 CCCN1CCCC(c2cccc(O)c2)C1 10.1021/jm00073a021
CHEMBL276500 105324 18 None -1 4 Human 6.9 pKi = 6.9 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 219 3 1 2 3.0 CCCN1CCCC(c2cccc(O)c2)C1 10.1021/jm00073a021
154724369 183468 1 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4584372 183468 1 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4598389 183468 1 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
127031829 146206 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793890 146206 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
127028182 146240 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
CHEMBL3794158 146240 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 336 5 0 4 3.2 Fc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)n1 10.1016/j.bmcl.2016.03.102
CHEMBL5290570 201282 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 334 4 1 6 2.1 CCOC(=O)c1sc2[nH]cn/c(=N\[C@H]3CCN(CC)C3)c2c1C 10.1016/j.ejmech.2020.113141
11370781 86646 0 None 14 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
CHEMBL212291 86646 0 None 14 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 325 6 0 6 2.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccnc1 10.1021/jm060279f
25071066 118551 0 None -18 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287390 118551 0 None -18 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c1Cl 10.1021/jm5004039
56837634 76081 0 None -295 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928130 76081 0 None -295 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
118709172 120196 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 493 8 0 4 6.6 Cc1ccc(C(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2014.06.079
CHEMBL3318844 120196 0 None -2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 493 8 0 4 6.6 Cc1ccc(C(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2014.06.079
137655029 165725 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 452 8 1 9 2.6 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4095881 165725 0 None -31 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 452 8 1 9 2.6 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
9995378 12245 0 None 25 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3ccc(-c4cnco4)c3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL107529 12245 0 None 25 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3ccc(-c4cnco4)c3)CC2)cc1 10.1016/s0960-894x(99)00540-5
276 10286 50 None -87 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptorDisplacement of [3H]spiperone from human cloned dopamine D4 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
5312149 10286 50 None -87 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptorDisplacement of [3H]spiperone from human cloned dopamine D4 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
CHEMBL431298 10286 50 None -87 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptorDisplacement of [3H]spiperone from human cloned dopamine D4 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
10476504 40261 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL142020 40261 1 None -1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
122189388 130021 0 None -25 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613874 130021 0 None -25 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
119570 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
2233 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
953 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
CHEMBL301265 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
DB00413 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
119570 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
2233 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
953 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
CHEMBL301265 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
DB00413 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
11077918 213373 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm015522j
CHEMBL88937 213373 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm015522j
11077918 213373 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm049612a
CHEMBL88937 213373 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm049612a
10021692 153160 19 None -1698 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 364 10 1 4 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL392158 153160 19 None -1698 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 364 10 1 4 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
11708363 78677 1 None -5 4 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm0503805
CHEMBL197159 78677 1 None -5 4 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm0503805
76336022 113156 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115581 113156 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139316 113156 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
136094866 47733 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 423 3 2 5 5.3 Cc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148694 47733 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 423 3 2 5 5.3 Cc1ccc2c(c1)C(NC1CC3CCC(C1)N3Cc1ccccc1)=Nc1cccnc1N2 10.1021/jm0104825
168285068 198362 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5195130 198362 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.ejmech.2022.114840
127051516 147635 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3819567 147635 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
56678599 73196 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 428 7 2 4 4.4 O=C1CCc2ccc(OCCCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813586 73196 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 428 7 2 4 4.4 O=C1CCc2ccc(OCCCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851900 73196 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 428 7 2 4 4.4 O=C1CCc2ccc(OCCCCN3CCC(O)(c4ccc(Cl)cc4)CC3)cc2N1 10.1016/j.bmc.2011.04.021
154725001 183426 1 None -85 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4525624 183426 1 None -85 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598002 183426 1 None -85 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
145980875 173486 0 None 3 11 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 443 7 1 2 6.2 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4282702 173486 0 None 3 11 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 443 7 1 2 6.2 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
127051516 147635 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3819567 147635 0 None -5 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 420 6 1 5 4.0 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3ccccc3s1)CC2 10.1016/j.bmc.2016.06.011
71062646 156322 0 None -218 13 Mouse 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3946661 156322 0 None -218 13 Mouse 6.9 pKi = 6.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
154727713 183143 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4514586 183143 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595727 183143 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
168287664 198431 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5196102 198431 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
154703922 183068 1 None -676 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4590211 183068 1 None -676 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595146 183068 1 None -676 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
44335972 116524 0 None 38 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.5 CC1Cc2ccccc2N1C(=O)CN1CCN(CCc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL323022 116524 0 None 38 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.5 CC1Cc2ccccc2N1C(=O)CN1CCN(CCc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44355355 30953 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL133938 30953 0 None 1 3 Human 6.9 pKi = 6.9 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
11849816 84854 0 None -5 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL210101 84854 0 None -5 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(\CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
168287664 198431 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5196102 198431 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
5249956 80170 1 None -70 6 Human 6.9 pKi = 6.9 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 80170 1 None -70 6 Human 6.9 pKi = 6.9 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
163322330 197479 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5182191 197479 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
168287664 198431 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5196102 198431 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3cn4ccccc4n3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
164611932 191981 0 None -33 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4857597 191981 0 None -33 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
168273063 197064 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5175728 197064 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)c1 10.1016/j.bmcl.2022.128615
11028157 209500 0 None -8 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/j.bmcl.2003.09.083
CHEMBL61789 209500 0 None -8 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/j.bmcl.2003.09.083
10183626 19820 0 None -44 3 Human 5.9 pKi = 5.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 0 4 6.2 Fc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1190010 19820 0 None -44 3 Human 5.9 pKi = 5.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 0 4 6.2 Fc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL539999 19820 0 None -44 3 Human 5.9 pKi = 5.9 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 0 4 6.2 Fc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
127052466 147564 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL3818669 147564 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
163322330 197479 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5182191 197479 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
163322330 197479 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5182191 197479 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
145968810 171817 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 171817 0 None -5 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
56658006 73144 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 468 7 2 5 4.4 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813588 73144 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 468 7 2 5 4.4 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851643 73144 0 None -4 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 468 7 2 5 4.4 O=C1CCc2ccc(OCCCCN3CCC(n4c(=O)[nH]c5cc(Cl)ccc54)CC3)cc2N1 10.1016/j.bmc.2011.04.021
44436300 155615 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL394110 155615 0 None -10 4 Human 6.9 pKi = 6.9 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 399 6 0 5 2.4 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2021.128028
44438206 153987 3 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 3 3 3 3.4 Oc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL392823 153987 3 None 3 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 3 3 3 3.4 Oc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
44336046 11577 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 398 4 0 2 3.6 C[C@@H]1CN(Cc2ccc(Cl)cc2)CC[N@@+]1(C)CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104138 11577 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 398 4 0 2 3.6 C[C@@H]1CN(Cc2ccc(Cl)cc2)CC[N@@+]1(C)CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
127052466 147564 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL3818669 147564 0 None -8 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 320 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1Cc2ccccc2C1 10.1016/j.bmc.2016.05.053
44332701 11335 0 None -35 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 360 8 2 5 2.9 CS(=O)(=O)Nc1cc(OCCNCc2cccs2)ccc1Cl 10.1016/s0960-894x(98)00014-6
CHEMBL102490 11335 0 None -35 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 360 8 2 5 2.9 CS(=O)(=O)Nc1cc(OCCNCc2cccs2)ccc1Cl 10.1016/s0960-894x(98)00014-6
10276451 207064 37 None -776 9 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL2112910 207064 37 None -776 9 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL59725 207064 37 None -776 9 Human 5.9 pKi = 5.9 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
73213196 111237 4 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 111237 4 None -12 13 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
44330514 215175 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 1 0 3 4.3 Cc1sc(C)c2c1CCCc1cnn(C(C)C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL99649 215175 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 1 0 3 4.3 Cc1sc(C)c2c1CCCc1cnn(C(C)C)c1-2 10.1016/s0960-894x(03)00587-0
119570 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 9933 96 None -6 39 Human 6.9 pKi = 6.9 Binding
in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
11026289 116311 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 425 6 1 4 3.8 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL322179 116311 0 None -3 3 Human 5.9 pKi = 5.9 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 425 6 1 4 3.8 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL5289845 201261 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 346 7 3 4 2.7 O=c1cc(CNC[C@@H](CO)Cc2ccsc2)[nH]c2ccc(F)cc12 10.1016/j.ejmech.2020.113141
155532148 178480 0 None -794 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(CC2COCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL4466677 178480 0 None -794 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(CC2COCC(c3ccccc3)(c3ccccc3)O2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL5082465 221583 0 None -239 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
44336062 11978 0 None 67 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL106119 11978 0 None 67 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
35296170 149118 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL388620 149118 3 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
49799695 21170 0 None -58 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1cccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1173436 21170 0 None -58 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1cccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1200285 21170 0 None -58 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1cccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL5090346 222036 0 None -11 4 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCc1ccccc1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
130431318 179162 2 None -1905 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 484 9 3 5 3.7 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4476394 179162 2 None -1905 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 484 9 3 5 3.7 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1 10.1021/acs.jmedchem.6b00860
168293190 198909 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5203595 198909 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 363 5 0 2 5.5 Cc1ccc(CO[C@H]2CCCN(Cc3ccc(Cl)c(Cl)c3)C2)cc1 10.1016/j.bmcl.2022.128615
11036641 38552 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL140612 38552 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
10473658 193972 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
CHEMBL49231 193972 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
44330567 215060 0 None 29 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 272 0 0 3 3.9 Cn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL98946 215060 0 None 29 2 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 272 0 0 3 3.9 Cn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
44336036 11648 0 None 416 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1CN(Cc2ccc(Cl)cc2)CCN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104399 11648 0 None 416 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1CN(Cc2ccc(Cl)cc2)CCN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
9841249 23167 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 348 3 0 4 3.7 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1C 10.1021/jm990266k
CHEMBL123030 23167 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 348 3 0 4 3.7 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1C 10.1021/jm990266k
9840412 124875 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 328 6 2 4 3.6 O=c1ccc2ccc(CNCCNc3ccc(Cl)cc3)cc2o1 10.1021/jm990266k
CHEMBL340669 124875 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 328 6 2 4 3.6 O=c1ccc2ccc(CNCCNc3ccc(Cl)cc3)cc2o1 10.1021/jm990266k
155538349 179155 0 None 43 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4476278 179155 0 None 43 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
145988180 172010 0 None -1 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4229178 172010 0 None -1 6 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
164628817 193056 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
CHEMBL4874069 193056 0 None -2 7 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 349 6 0 4 3.4 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc2c(c1)CCC2 10.1016/j.ejmech.2021.113243
56944383 118896 0 None -25 12 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 118896 0 None -25 12 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
44405455 79143 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 398 5 1 3 4.7 O=C(N[C@H]1CCN(Cc2ccc(F)c(F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL198580 79143 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 398 5 1 3 4.7 O=C(N[C@H]1CCN(Cc2ccc(F)c(F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
44405489 139594 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL370134 139594 0 None 9 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
44405466 173159 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 392 6 1 4 4.4 COc1cccc(CN2CC[C@H](NC(=O)c3ccc(-c4cccs4)cc3)C2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL427555 173159 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 392 6 1 4 4.4 COc1cccc(CN2CC[C@H](NC(=O)c3ccc(-c4cccs4)cc3)C2)c1 10.1016/j.bmcl.2005.08.051
53364083 70628 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 658 21 0 11 6.2 CCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803053 70628 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 658 21 0 11 6.2 CCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
72545011 99901 0 None 8 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443004 99901 0 None 8 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
137636460 162899 0 None 2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063282 162899 0 None 2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
137642380 165286 0 None -2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4091155 165286 0 None -2 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
11036641 38552 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL140612 38552 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
71734029 97830 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
CHEMBL2397392 97830 0 None -4 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
45272537 203305 0 None 181 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL563614 203305 0 None 181 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
44393775 73078 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
CHEMBL184853 73078 0 None - 1 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
10200496 90368 0 None -25 5 Human 7.9 pKi = 7.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
CHEMBL2204343 90368 0 None -25 5 Human 7.9 pKi = 7.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
10473658 193972 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49231 193972 3 None 38 3 Human 7.9 pKi = 7.9 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
9909055 11614 4 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 401 4 0 4 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCSc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104238 11614 4 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 401 4 0 4 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCSc2ccccc21 10.1016/s0960-894x(02)00655-8
11325334 86826 0 None 11 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212969 86826 0 None 11 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
127031515 146212 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793910 146212 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
76314268 113211 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115577 113211 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 113211 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
18414156 113863 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
CHEMBL315864 113863 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
18414156 113863 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1007/s00044-012-0055-5
CHEMBL315864 113863 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 308 3 2 4 2.6 Oc1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1007/s00044-012-0055-5
76314268 113211 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115577 113211 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 113211 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
11724450 130626 4 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 130626 4 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 130626 4 None - 1 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
2728532 118331 3 None -1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 291 3 1 2 3.5 c1ccc(CN2CCN(c3cccc4[nH]ccc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
CHEMBL328051 118331 3 None -1 4 Human 7.8 pKi = 7.8 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 291 3 1 2 3.5 c1ccc(CN2CCN(c3cccc4[nH]ccc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
76331467 92660 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 287 3 1 0 2.8 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]ccc34)cc2)cc1 10.1007/s00044-012-0055-5
CHEMBL2298808 92660 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 287 3 1 0 2.8 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]ccc34)cc2)cc1 10.1007/s00044-012-0055-5
10064981 211807 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL76982 211807 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
44264629 104141 0 None 33 4 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4c3ccc3ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL269576 104141 0 None 33 4 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4c3ccc3ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44380685 65509 0 None 4 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL168566 65509 0 None 4 4 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
25128757 110081 0 None -38 6 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
CHEMBL3084512 110081 0 None -38 6 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
134154387 159239 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3970994 159239 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL5272829 200516 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 320 6 1 3 3.8 CCS[C@H]1CC[C@@H](N(C)CC(=O)Nc2ccc(C)c(C)c2)C1 10.1016/j.ejmech.2020.113141
164626655 193372 0 None -41 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4878587 193372 0 None -41 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
145990141 173558 0 None -67 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 388 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Cl)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4283982 173558 0 None -67 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 388 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Cl)cc1)CC2 10.1021/acsmedchemlett.8b00229
60167309 82072 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL2037432 82072 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
60167309 82072 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.ejmech.2012.03.042
CHEMBL2037432 82072 0 None -1 7 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.ejmech.2012.03.042
11699469 84427 0 None -8 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 537 8 1 5 5.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3c4ccc(c3o2)CCc2ccc(cc2)CC4)CC1 10.1021/jm060138d
CHEMBL208847 84427 0 None -8 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 537 8 1 5 5.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3c4ccc(c3o2)CCc2ccc(cc2)CC4)CC1 10.1021/jm060138d
57402365 76070 0 None -10 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928119 76070 0 None -10 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
56837635 76083 0 None -467 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928132 76083 0 None -467 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
57398875 76089 0 None -40 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928138 76089 0 None -40 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
127046950 146823 0 None -7 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800303 146823 0 None -7 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137643122 164814 0 None -17 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4085752 164814 0 None -17 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
44459452 100668 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1cc(-c2ccccc2)n(C2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(99)00169-9
CHEMBL24809 100668 0 None 2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1cc(-c2ccccc2)n(C2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(99)00169-9
19964406 121293 2 None 75 2 Human 6.9 pKi = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335535 121293 2 None 75 2 Human 6.9 pKi = 6.9 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CCC2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
10524751 64128 0 None 1 4 Human 5.9 pKi = 5.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 395 5 0 1 6.5 CCCN(CCC)C1CCC(=C(C#Cc2ccccc2)C#Cc2ccccc2)CC1 10.1021/jm991098z
CHEMBL165171 64128 0 None 1 4 Human 5.9 pKi = 5.9 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 395 5 0 1 6.5 CCCN(CCC)C1CCC(=C(C#Cc2ccccc2)C#Cc2ccccc2)CC1 10.1021/jm991098z
10543696 11353 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4ccncn4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL102599 11353 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4ccncn4)CC3)c[nH]2)cc1 10.1021/jm960637m
51354277 66987 0 None -1288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 429 11 1 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1688992 66987 0 None -1288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 429 11 1 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1739996 66987 0 None -1288 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 429 11 1 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCF)cc2)CC1 10.1021/jm101323b
145993220 173543 0 None -58 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 355 7 2 5 2.4 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccncc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4283709 173543 0 None -58 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 355 7 2 5 2.4 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccncc1)CC2 10.1021/acsmedchemlett.8b00229
168277992 196907 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5173368 196907 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
168277992 196907 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5173368 196907 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
25139332 191098 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
CHEMBL484204 191098 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
127045853 146571 0 None -5623 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3798748 146571 0 None -5623 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
118709168 120192 0 None -7 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1000 29 0 8 14.4 O=C(CCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318840 120192 0 None -7 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1000 29 0 8 14.4 O=C(CCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
122189389 130022 0 None -323 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613875 130022 0 None -323 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
11694483 79018 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 249 6 0 4 2.1 CCCN(CCC)C1CCn2ncc(C=O)c2C1 10.1021/jm0503805
CHEMBL198174 79018 0 None -2 3 Human 4.9 pKi = 4.9 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 249 6 0 4 2.1 CCCN(CCC)C1CCn2ncc(C=O)c2C1 10.1021/jm0503805
90644069 118815 0 None -1 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 341 4 0 4 3.8 Clc1ccc(N2CCN(CCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289651 118815 0 None -1 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 341 4 0 4 3.8 Clc1ccc(N2CCN(CCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
60165537 82126 0 None -1 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 308 5 0 3 4.6 c1ccc2c(c1)CN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
CHEMBL2037523 82126 0 None -1 4 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 308 5 0 3 4.6 c1ccc2c(c1)CN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
10548967 119508 0 None -12 3 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1ccc2c(c1)C(=O)N(CCN1CCN(c3ccc(Cl)cc3)CC1)CC2 10.1021/jm991138z
CHEMBL330470 119508 0 None -12 3 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1ccc2c(c1)C(=O)N(CCN1CCN(c3ccc(Cl)cc3)CC1)CC2 10.1021/jm991138z
134154387 159239 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3970994 159239 0 None -2 9 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 289 3 0 1 4.5 C1=C(CCN2CCc3ccccc3C2)CCc2ccccc21 10.1016/j.bmc.2016.09.019
60167309 82072 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL2037432 82072 0 None 1 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 400 6 1 4 5.3 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
168277992 196907 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5173368 196907 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1cnc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
154724650 183116 1 None -79 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4543870 183116 1 None -79 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595492 183116 1 None -79 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
44192200 202168 2 None -380 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 451 3 0 7 3.9 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C#N)ccc4n2)CC1)O3 10.1021/jm900374r
CHEMBL551964 202168 2 None -380 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 451 3 0 7 3.9 Cc1ccc2c3c(ccc2n1)OC[C@H](CN1CCN(c2ccc4cc(C#N)ccc4n2)CC1)O3 10.1021/jm900374r
44396235 175316 1 None -91 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL435505 175316 1 None -91 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
164622973 192902 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4871868 192902 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
155564667 182260 0 None -154 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 459 8 1 6 4.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc4sccn4c3C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4577414 182260 0 None -154 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 459 8 1 6 4.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc4sccn4c3C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4444356 220711 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None Nc1ccc(CN2CCC(n3cc(Cc4ccc(Br)cc4)nn3)CC2)cc1 10.1016/j.bmc.2022.116851
9926401 147653 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819556 147653 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819732 147653 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
16094676 7020 19 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
8439 7020 19 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
CHEMBL219182 7020 19 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 10.1021/jm060662k
5493357 213605 4 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 2 1 4 3.4 Cc1cc(O)c2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL90466 213605 4 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 321 2 1 4 3.4 Cc1cc(O)c2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
9952218 11653 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(F)cccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104432 11653 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(F)cccc21 10.1016/s0960-894x(02)00655-8
90644065 118438 0 None 1 4 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 355 5 0 4 4.2 Clc1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3286429 118438 0 None 1 4 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 355 5 0 4 4.2 Clc1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
12050194 209670 1 None 5 4 Human 5.8 pKi = 5.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 333 5 0 4 3.7 c1ccc(CN2CCN(Cc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL62703 209670 1 None 5 4 Human 5.8 pKi = 5.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 333 5 0 4 3.7 c1ccc(CN2CCN(Cc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
9926401 147653 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819556 147653 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819732 147653 0 None -2 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 301 5 0 2 4.4 Fc1ccc(SCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
71061709 156306 0 None 3 12 Mouse 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3946540 156306 0 None 3 12 Mouse 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
164611932 191981 0 None -33 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4857597 191981 0 None -33 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 364 6 1 4 3.1 O=C1CCc2cc(CCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
44427842 156587 0 None -9 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 494 7 1 4 5.2 O=C(NC[C@H]1C[C@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL394863 156587 0 None -9 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 494 7 1 4 5.2 O=C(NC[C@H]1C[C@H]1CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
168269421 196741 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5170670 196741 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.ejmech.2022.114840
49862238 21780 16 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 367 6 0 5 3.6 COc1cccc(F)c1OC1CN(Cc2cnn(-c3ccccc3)c2C)C1 10.1016/j.bmcl.2010.06.033
CHEMBL1209158 21780 16 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 367 6 0 5 3.6 COc1cccc(F)c1OC1CN(Cc2cnn(-c3ccccc3)c2C)C1 10.1016/j.bmcl.2010.06.033
5249956 80170 1 None -70 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
CHEMBL201525 80170 1 None -70 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
44278111 106908 0 None 13 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 368 4 1 3 4.6 c1ccc(-c2ccc(N3CCN(Cc4c[nH]c5ncccc45)CC3)cc2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL287671 106908 0 None 13 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 368 4 1 3 4.6 c1ccc(-c2ccc(N3CCN(Cc4c[nH]c5ncccc45)CC3)cc2)cc1 10.1016/s0960-894x(01)00241-4
11957566 6972 25 None -43 8 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
1219 6972 25 None -43 8 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
3296 6972 25 None -43 8 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
950 6972 25 None -43 8 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
CHEMBL285755 6972 25 None -43 8 Human 6.8 pKi = 6.8 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/S0960-894X(97)10068-3
168269421 196741 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5170670 196741 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.ejmech.2022.114840
168269421 196741 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170670 196741 0 None 6 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 390 5 1 2 5.3 Fc1ccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)cc1F 10.1016/j.bmcl.2022.128615
53248212 68807 0 None -154 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
CHEMBL1774534 68807 0 None -154 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 424 8 2 4 3.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm200288r
44427831 99014 0 None -338 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 460 9 2 6 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
CHEMBL242644 99014 0 None -338 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 460 9 2 6 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2ccc(-c3ccccn3)cc2)CC1 10.1021/jm0704200
44438209 160741 0 None -9 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 406 9 2 3 5.6 CCCCCCOc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL398368 160741 0 None -9 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 406 9 2 3 5.6 CCCCCCOc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
9888555 172383 16 None -208 8 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
CHEMBL424294 172383 16 None -208 8 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
10642239 193438 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL48819 193438 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity to human dopamine D4.4 receptor by radioligand displacement assayBinding affinity to human dopamine D4.4 receptor by radioligand displacement assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.01.044
44335907 12151 0 None 14 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107020 12151 0 None 14 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 417 4 0 3 4.1 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
44335800 116824 0 None 138 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL323525 116824 0 None 138 2 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
155537361 179077 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 541 10 2 5 5.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4475042 179077 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 541 10 2 5 5.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2Cl)CC1 10.1021/acs.jmedchem.9b01085
155542182 179888 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 516 10 2 6 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4520460 179888 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 516 10 2 6 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(C#N)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
71449737 88600 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 468 7 0 7 3.5 COc1ccccc1N1CCN(CCN(C(=O)c2cnc3ccccc3n2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
CHEMBL2164349 88600 0 None -6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 468 7 0 7 3.5 COc1ccccc1N1CCN(CCN(C(=O)c2cnc3ccccc3n2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
44405452 79331 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.7 O=C(N[C@H]1CCN(Cc2ccc(Cl)c(Cl)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL199186 79331 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.7 O=C(N[C@H]1CCN(Cc2ccc(Cl)c(Cl)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
53361301 70616 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803024 70616 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
21219154 95338 0 None 33 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3nccc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL23537 95338 0 None 33 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3nccc3-c3ccccc3)CC2)cc1 10.1016/s0960-894x(99)00169-9
56926587 75785 0 None 380 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 329 3 0 5 2.3 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cn1 10.1021/jm200762g
CHEMBL1923416 75785 0 None 380 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 329 3 0 5 2.3 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cn1 10.1021/jm200762g
53361301 70616 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL1803024 70616 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
10642239 193438 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48819 193438 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
10642239 193438 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48819 193438 1 None 53 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
9888555 172383 16 None -208 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm0611152
CHEMBL424294 172383 16 None -208 8 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm0611152
9861786 119122 0 None -19 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 317 6 3 4 3.1 Oc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL329398 119122 0 None -19 4 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 317 6 3 4 3.1 Oc1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
44273855 81177 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 381 7 1 4 3.4 COc1cc(Cl)ccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20251 81177 0 None 10 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 381 7 1 4 3.4 COc1cc(Cl)ccc1N1CCN(CCCCNC(=O)C(C)(C)C)CC1 10.1016/0960-894X(96)00198-9
44273928 84856 0 None 63 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21011 84856 0 None 63 2 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
10665101 108302 0 None 22 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL298166 108302 0 None 22 3 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
10413085 89965 0 None -64 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 484 8 2 4 4.3 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0611152
CHEMBL218444 89965 0 None -64 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 484 8 2 4 4.3 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3[nH]2)CC1 10.1021/jm0611152
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00200-1
127032383 146181 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793438 146181 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
10852461 213742 2 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 310 4 2 3 2.9 O=C(Nc1ccccn1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91272 213742 2 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 310 4 2 3 2.9 O=C(Nc1ccccn1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10449136 214210 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL94067 214210 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10053476 123524 0 None -275 5 Human 6.8 pKi = 6.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 559 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[te]1 10.1021/jm025558r
CHEMBL337531 123524 0 None -275 5 Human 6.8 pKi = 6.8 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 559 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[te]1 10.1021/jm025558r
44380802 168470 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL413343 168470 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
127053220 146145 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL3793062 146145 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 319 5 0 3 3.2 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2016.03.102
CHEMBL5277325 200711 0 None 35 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 343 7 2 2 3.5 CN(C)[C@@H](CNC(=O)NC[C@H]1Cc2ccccc21)CC1CCCCC1 10.1016/j.ejmech.2020.113141
11849821 176079 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL441529 176079 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 374 6 1 6 2.3 CO/N=C(/c1ccc(Cl)cc1)C(O)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
145991769 173660 0 None -12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1cccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)c1 10.1021/acsmedchemlett.8b00229
CHEMBL4285984 173660 0 None -12 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1cccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)c1 10.1021/acsmedchemlett.8b00229
10476504 40261 1 None -1 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
CHEMBL142020 40261 1 None -1 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
72545007 99897 0 None 3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443000 99897 0 None 3 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
71456214 85461 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 450 8 1 4 4.7 CCCNC(=O)c1cc(C)c(OCC2CN(Cc3ccc(Cl)cc3)CCO2)cc1Cl 10.1021/jm031111m
CHEMBL2112466 85461 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 450 8 1 4 4.7 CCCNC(=O)c1cc(C)c(OCC2CN(Cc3ccc(Cl)cc3)CCO2)cc1Cl 10.1021/jm031111m
71457956 85199 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111527 85199 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
71454405 85200 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL2111528 85200 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
44340415 15350 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL109472 15350 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
72205044 98720 0 None -4 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 410 8 0 5 4.3 Clc1ccc(-n2cc(COCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414355 98720 0 None -4 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 410 8 0 5 4.3 Clc1ccc(-n2cc(COCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
145979897 173385 0 None -151 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 480 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(I)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4280542 173385 0 None -151 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 480 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(I)cc1)CC2 10.1021/acsmedchemlett.8b00229
15508243 12075 22 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 366 3 0 2 3.9 Ic1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL106635 12075 22 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 366 3 0 2 3.9 Ic1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
10682854 31408 1 None -2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL134326 31408 1 None -2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
44419056 89952 0 None -398 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)sc2c1 10.1021/jm0611152
CHEMBL218368 89952 0 None -398 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)sc2c1 10.1021/jm0611152
9930722 210451 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL67414 210451 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
9930722 210451 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(02)01056-9
CHEMBL67414 210451 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 397 4 0 3 3.8 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(02)01056-9
127050632 147521 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818124 147521 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
168282745 197874 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5187721 197874 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
12581156 31922 17 None -8 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 1 2 2.2 CCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL134759 31922 17 None -8 3 Human 5.8 pKi = 5.8 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 1 2 2.2 CCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
72164183 98926 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420778 98926 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
133633 9021 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
177 9021 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
CHEMBL445102 9021 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmcl.2006.10.076
155195311 181126 0 None -208 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4551160 181126 0 None -208 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
133633 9021 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2008.12.054
177 9021 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2008.12.054
CHEMBL445102 9021 53 None -104 8 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2008.12.054
44438235 100433 2 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 353 4 1 4 4.6 CSc1ccc(C2(O)CCN(Cc3coc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL246854 100433 2 None -2 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 353 4 1 4 4.6 CSc1ccc(C2(O)CCN(Cc3coc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
42626381 63019 0 None -645 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 452 9 3 6 2.5 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm900095y
CHEMBL1627315 63019 0 None -645 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 452 9 3 6 2.5 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm900095y
44431473 157518 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2006.12.106
CHEMBL395632 157518 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2cccc3ccccc23)CC1 10.1016/j.bmcl.2006.12.106
44438197 160051 2 None -58 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL397770 160051 2 None -58 3 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
44304814 209651 0 None -2 4 Human 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 505 8 1 5 5.9 COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12 10.1016/s0960-894x(00)00405-4
CHEMBL62601 209651 0 None -2 4 Human 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 505 8 1 5 5.9 COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12 10.1016/s0960-894x(00)00405-4
CHEMBL5270705 200424 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 344 5 0 7 2.4 Cc1csc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)n1 10.1016/j.ejmech.2022.114840
44330564 114159 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 1 0 3 5.0 CC(C)n1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL317825 114159 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 1 0 3 5.0 CC(C)n1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
44336057 12680 0 None 2 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 437 4 0 3 4.8 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCCC2 10.1016/s0960-894x(02)00655-8
CHEMBL107962 12680 0 None 2 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 437 4 0 3 4.8 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCCC2 10.1016/s0960-894x(02)00655-8
168297637 199102 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5206427 199102 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
9801858 70220 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CCC2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL179757 70220 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CCC2C1)c1ccc2ccccc2c1 10.1021/jm049031l
9817612 114033 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 294 1 0 3 4.7 Cc1sc(C)c2c1CCCc1cnn(-c3ccccc3)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL316942 114033 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 294 1 0 3 4.7 Cc1sc(C)c2c1CCCc1cnn(-c3ccccc3)c1-2 10.1016/s0960-894x(03)00587-0
168297637 199102 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5206427 199102 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
44273876 86590 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 371 7 1 3 3.7 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/0960-894X(96)00198-9
CHEMBL21205 86590 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 371 7 1 3 3.7 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/0960-894X(96)00198-9
44517726 202801 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to DAD4 receptorBinding affinity to DAD4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.07.055
CHEMBL560177 202801 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to DAD4 receptorBinding affinity to DAD4 receptor
ChEMBL 341 4 0 2 3.6 O=C1N(CCN2Cc3ccccc3C2)CCN1c1cccc(Cl)c1 10.1016/j.bmcl.2009.07.055
168297637 199102 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5206427 199102 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 4 4.3 Fc1cc(COC2CCN(Cc3ncc4ccccn34)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
164622973 192902 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4871868 192902 0 None -61 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 397 6 0 4 4.5 CC1(CCCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
127051015 147652 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 147652 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 147652 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
11576528 91096 0 None -32 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 476 11 1 7 3.4 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
CHEMBL221587 91096 0 None -32 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 476 11 1 7 3.4 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
9952528 106214 0 None -1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 394 5 1 3 3.8 NC(=O)C1CCC(CN2CCC(=C(c3ccccc3)c3ccc(F)cc3)CC2)O1 10.1016/s0960-894x(01)00200-1
CHEMBL282927 106214 0 None -1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity for Dopamine receptor D4In vitro binding affinity for Dopamine receptor D4
ChEMBL 394 5 1 3 3.8 NC(=O)C1CCC(CN2CCC(=C(c3ccccc3)c3ccc(F)cc3)CC2)O1 10.1016/s0960-894x(01)00200-1
11191906 18539 0 None -31 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181665 18539 0 None -31 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL187928 18539 0 None -31 12 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL5270705 200424 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 344 5 0 7 2.4 Cc1csc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)n1 10.1016/j.ejmech.2022.114840
127050632 147521 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
CHEMBL3818124 147521 0 None -87 9 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 6 1 5 4.7 O=C1NCN(c2ccccc2)C12CCN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.06.011
126534204 145210 0 None -1412 5 Human 4.8 pKi = 4.8 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
CHEMBL3774411 145210 0 None -1412 5 Human 4.8 pKi = 4.8 Binding
Binding affinity to dopamine D4 receptor (unknown origin)Binding affinity to dopamine D4 receptor (unknown origin)
ChEMBL 504 7 1 7 3.9 Cn1c(SCCCN2CC3CCN(c4ccc(C(F)(F)F)cc4)C3C2)nnc1-c1cc[nH]c(=O)c1 10.1016/j.bmc.2016.02.031
154705884 183142 1 None -48 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4469584 183142 1 None -48 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595726 183142 1 None -48 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
71658072 97173 0 None -18 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 399 8 1 4 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386611 97173 0 None -18 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 399 8 1 4 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmc.2013.03.074
44374431 61726 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 261 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL161507 61726 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 261 4 1 3 2.9 CCCN[C@@H]1CCc2c(C(=O)OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970170v
10665626 119349 0 None 41 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc2c3c(c(=O)oc2c1OC)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL330100 119349 0 None 41 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc2c3c(c(=O)oc2c1OC)CN(Cc1ccccc1)CC3 10.1021/jm970170v
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
16104 168696 19 None -1 5 Human 7.8 pKi = 7.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL415300 168696 19 None -1 5 Human 7.8 pKi = 7.8 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
5311189 211620 11 None -1 27 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
CHEMBL7549 211620 11 None -1 27 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 16/1300)
ChEMBL 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 10.1016/s0960-894x(02)00390-6
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970422s
2389 10104 118 None -22 66 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
5073 10104 118 None -22 66 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
96 10104 118 None -22 66 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
CHEMBL85 10104 118 None -22 66 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
DB00734 10104 118 None -22 66 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
2389 10104 118 None -22 66 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
5073 10104 118 None -22 66 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
96 10104 118 None -22 66 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
CHEMBL85 10104 118 None -22 66 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
DB00734 10104 118 None -22 66 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
9906071 23079 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 342 6 2 4 4.0 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1Cl 10.1021/jm990266k
CHEMBL122597 23079 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 342 6 2 4 4.0 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1Cl 10.1021/jm990266k
10854185 121317 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3ccc(=O)oc3c2)CC1 10.1021/jm990266k
CHEMBL333658 121317 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3ccc(=O)oc3c2)CC1 10.1021/jm990266k
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cellsCompetitive binding affinity against human Dopamine receptor D4 by displacing [3H]spiperone from CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
155518026 177016 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 528 11 2 7 4.0 COc1ccc(N(Cc2ccc(C#N)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4445706 177016 0 None 10 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 528 11 2 7 4.0 COc1ccc(N(Cc2ccc(C#N)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
162653993 190447 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4753809 190447 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802865 190447 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
3645619 9808 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
975 9808 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
CHEMBL45244 9808 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.ejmech.2020.113141
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.113141
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.113141
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.113141
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.113141
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2020.113141
3251 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
5684 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
80 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
CHEMBL31354 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.ejmech.2011.06.023
127052487 147578 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818805 147578 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
25070740 118552 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccn4nccc34)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287391 118552 0 None -1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccn4nccc34)CC2)c1Cl 10.1021/jm5004039
25072943 118554 0 None -2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccc4ccnn34)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287393 118554 0 None -2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cccc4ccnn34)CC2)c1Cl 10.1021/jm5004039
44431486 94848 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL234645 94848 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)c1 10.1016/j.bmcl.2006.12.106
44405469 78761 0 None 14 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 396 5 1 3 5.1 O=C(N[C@H]1CCN(Cc2ccc(Cl)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL197381 78761 0 None 14 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 396 5 1 3 5.1 O=C(N[C@H]1CCN(Cc2ccc(Cl)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
72545240 99904 0 None 16 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443007 99904 0 None 16 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
44436602 151991 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL391256 151991 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 391 8 1 4 3.0 C#Cc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2007.08.038
2 10035 23 None -2 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
54562 10035 23 None -2 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
CHEMBL240773 10035 23 None -2 28 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
122181329 128648 0 None -51 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590080 128648 0 None -51 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
71459759 90846 0 None 4 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 432 4 0 3 5.5 COc1ccccc1N1CCN(Cc2cc(C#Cc3ccccc3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207633 90846 0 None 4 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 432 4 0 3 5.5 COc1ccccc1N1CCN(Cc2cc(C#Cc3ccccc3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
45269168 202709 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 1 6 2.3 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(F)cc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL559399 202709 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 410 4 1 6 2.3 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(F)cc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
3251 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
5684 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
80 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
CHEMBL31354 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
127031519 146101 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792638 146101 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 329 6 0 4 3.7 CSc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127053221 146109 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3792728 146109 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
127052487 147578 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818805 147578 0 None 3 6 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 422 6 2 3 5.1 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2016.06.011
10612157 108634 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1021/jm9703653
CHEMBL300571 108634 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1021/jm9703653
CHEMBL423890 108634 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1021/jm9703653
10612157 108634 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1016/s0960-894x(98)00014-6
CHEMBL300571 108634 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1016/s0960-894x(98)00014-6
CHEMBL423890 108634 1 None -15 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 271 4 2 4 2.3 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CO2 10.1016/s0960-894x(98)00014-6
162653993 190447 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4753809 190447 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802865 190447 0 None 1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3cccnc3)CC2)cc1 10.1016/j.bmc.2020.115943
3645619 9808 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
975 9808 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
CHEMBL45244 9808 20 None -5 9 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
9982854 91115 0 None -24 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 485 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3o2)CC1 10.1021/jm0611152
CHEMBL221681 91115 0 None -24 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 485 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(Br)ccc3o2)CC1 10.1021/jm0611152
10687967 211831 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 331 5 1 2 4.4 c1ccc(Cc2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL77148 211831 0 None 1 3 Human 6.8 pKi = 6.8 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 331 5 1 2 4.4 c1ccc(Cc2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
10039198 63123 0 None -4 4 Human 6.8 pKi = 6.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 63123 0 None -4 4 Human 6.8 pKi = 6.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
15467372 175889 0 None 43 4 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(99)00302-9
CHEMBL440120 175889 0 None 43 4 Human 6.8 pKi = 6.8 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(99)00302-9
127032082 146095 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792541 146095 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127051015 147652 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818128 147652 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819731 147652 0 None -5 9 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 283 5 0 1 4.2 Fc1ccc(CCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
137635364 163039 0 None -512 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4064974 163039 0 None -512 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4074669 163039 0 None -512 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
57391896 76080 0 None -24 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928129 76080 0 None -24 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
57400557 76087 0 None -131 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928136 76087 0 None -131 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
118709170 120194 0 None -6 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1057 33 0 8 16.0 O=C(CCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318842 120194 0 None -6 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1057 33 0 8 16.0 O=C(CCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137645830 164631 0 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
CHEMBL4083727 164631 0 None -3 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
10924369 16108 1 None -1000 6 Human 6.8 pKi = 6.8 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@@H]1c1ccccc1C2 10.1021/jm010566d
CHEMBL111184 16108 1 None -1000 6 Human 6.8 pKi = 6.8 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@@H]1c1ccccc1C2 10.1021/jm010566d
11747350 114109 0 None -79 10 Human 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligandBinding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligand
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
CHEMBL317535 114109 0 None -79 10 Human 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligandBinding affinity against dopamine receptor D4 cloned in HEK 293 cells using [3H]spiperone radioligand
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
2337 10030 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
50 10030 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
5002 10030 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
CHEMBL716 10030 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
DB01224 10030 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
2337 10030 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
50 10030 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
5002 10030 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
CHEMBL716 10030 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
DB01224 10030 77 None -114 62 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
CHEMBL5075726 221174 0 None -30 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/acs.jmedchem.1c00611
44335635 11568 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104099 11568 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
44381217 65920 0 None 4 4 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL169889 65920 0 None 4 4 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
44319368 112841 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
CHEMBL313320 112841 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
11356479 78612 0 None -8 3 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
CHEMBL196928 78612 0 None -8 3 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
10564794 64313 0 None -4 3 Human 4.8 pKi = 4.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 281 5 0 1 4.6 CCCN(CCC)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm991098z
CHEMBL166325 64313 0 None -4 3 Human 4.8 pKi = 4.8 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 281 5 0 1 4.6 CCCN(CCC)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm991098z
11615782 79001 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 251 6 1 4 1.8 CCCN(CCC)C1CCn2ncc(CO)c2C1 10.1021/jm0503805
CHEMBL198125 79001 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 251 6 1 4 1.8 CCCN(CCC)C1CCn2ncc(CO)c2C1 10.1021/jm0503805
154704368 183250 1 None -35 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4569006 183250 1 None -35 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596571 183250 1 None -35 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
135469096 18838 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 366 6 1 7 2.1 c1cnc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183656 18838 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 366 6 1 7 2.1 c1cnc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL309843 18838 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 366 6 1 7 2.1 c1cnc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
71658074 97175 0 None -64 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 420 8 2 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386613 97175 0 None -64 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 420 8 2 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1016/j.bmc.2013.03.074
76325764 113077 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 434 8 2 5 3.3 COc1ccc2[nH]c(C(=O)NC/C=C/CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1039/c3md00098b
CHEMBL3133866 113077 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 434 8 2 5 3.3 COc1ccc2[nH]c(C(=O)NC/C=C/CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1039/c3md00098b
CHEMBL3139064 113077 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 434 8 2 5 3.3 COc1ccc2[nH]c(C(=O)NC/C=C/CN3CCN(c4ccccc4OC)CC3)cc2c1 10.1039/c3md00098b
60167452 82129 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037526 82129 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
60167452 82129 0 None -9 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037526 82129 0 None -9 8 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
4064333 92515 19 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
4064333 92515 19 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL229019 92515 19 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL229019 92515 19 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(NC1CCN(Cc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
3038495 7495 37 None -109 18 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
7625 7495 37 None -109 18 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
CHEMBL25236 7495 37 None -109 18 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm049031l
60167452 82129 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037526 82129 0 None -9 8 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 448 7 1 6 4.1 O=C(CCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
127051016 147654 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819642 147654 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819734 147654 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
49798839 21134 0 None -53 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 347 3 1 4 3.9 O=c1[nH]c2ccccc2n1C1CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172214 21134 0 None -53 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 347 3 1 4 3.9 O=c1[nH]c2ccccc2n1C1CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200154 21134 0 None -53 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 347 3 1 4 3.9 O=c1[nH]c2ccccc2n1C1CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
154703438 183160 1 None -6 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4475699 183160 1 None -6 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4595859 183160 1 None -6 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
127051016 147654 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819642 147654 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819734 147654 0 None -5 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 386 5 1 4 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
118719799 122504 0 None -25 4 Human 6.8 pKi = 6.8 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 487 10 0 7 5.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353902 122504 0 None -25 4 Human 6.8 pKi = 6.8 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 487 10 0 7 5.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
10893228 46988 0 None 117 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 0 1 5 3.5 CN1CCCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
CHEMBL148042 46988 0 None 117 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 0 1 5 3.5 CN1CCCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
145970938 171935 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4228054 171935 0 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
145992489 173756 0 None -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4287623 173756 0 None -5 12 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 535 7 1 2 7.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
9992499 80161 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
CHEMBL201483 80161 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
168283295 198014 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL5189986 198014 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.ejmech.2022.114840
11566745 81469 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL1202298 81469 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL203029 81469 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
168283295 198014 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
CHEMBL5189986 198014 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.bmcl.2022.128615
168275962 197398 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5180979 197398 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)ccc1F 10.1016/j.bmcl.2022.128615
168291848 198651 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5199552 198651 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3ncn4ccccc34)CC2)c1 10.1016/j.bmcl.2022.128615
168283295 198014 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL5189986 198014 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 327 5 0 2 4.6 Cc1ccc(CN2CCC[C@H](OCc3ccc(F)c(C)c3)C2)cc1 10.1016/j.ejmech.2022.114840
168275089 197275 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5179198 197275 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
71061729 167722 0 None 1 4 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4115493 167722 0 None 1 4 Mouse 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
5025739 175975 45 None 30 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
CHEMBL440687 175975 45 None 30 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm0305669
44438233 100385 2 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 1 3 5.2 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246643 100385 2 None -7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 1 3 5.2 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
168279825 197595 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5183902 197595 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.bmcl.2022.128615
44426511 144072 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(c1ccc2ccccc2c1)N1CCC(NCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL375238 144072 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 344 4 1 2 4.2 O=C(c1ccc2ccccc2c1)N1CCC(NCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
44330566 215059 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 286 1 0 3 4.4 CCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL98945 215059 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 286 1 0 3 4.4 CCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
11133533 51991 0 None -13 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 418 8 1 5 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3nccc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL152587 51991 0 None -13 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 418 8 1 5 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3nccc4ccccc34)CC2)c1 10.1021/jm020952a
242 7258 124 None -104 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
34 7258 124 None -104 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
60795 7258 124 None -104 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
CHEMBL1112 7258 124 None -104 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
DB01238 7258 124 None -104 51 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2011.04.021
11849736 145193 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377388 145193 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 344 7 0 6 3.1 CCO/N=C(\CCN1CCN(c2nccs2)CC1)c1ccccc1 10.1021/jm060279f
44431471 175157 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL434583 175157 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
155195496 177495 0 None -72 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4452064 177495 0 None -72 3 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
122442272 145126 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 145126 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 145126 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
44330386 114151 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 258 0 1 2 3.9 Clc1sc(Cl)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317770 114151 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 258 0 1 2 3.9 Clc1sc(Cl)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL5270836 200435 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 377 5 1 5 3.9 Cc1csc(OC[C@@H]2CN(Cc3cc4ccc(Cl)cc4[nH]3)CCO2)n1 10.1016/j.ejmech.2022.114840
5311346 210933 28 None -19 5 Human 6.8 pKi = 6.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL1256778 210933 28 None -19 5 Human 6.8 pKi = 6.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL70565 210933 28 None -19 5 Human 6.8 pKi = 6.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
168292124 198804 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5201917 198804 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 365 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(F)c(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
168290895 198778 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5201507 198778 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5270836 200435 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 377 5 1 5 3.9 Cc1csc(OC[C@@H]2CN(Cc3cc4ccc(Cl)cc4[nH]3)CCO2)n1 10.1016/j.ejmech.2022.114840
11453253 91089 0 None -54 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 9 1 5 3.7 COc1ccc(C(=O)NCCCCN2CCN(c3ccccc3Cl)CC2)cc1OC 10.1021/jm0611152
CHEMBL221549 91089 0 None -54 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 9 1 5 3.7 COc1ccc(C(=O)NCCCCN2CCN(c3ccccc3Cl)CC2)cc1OC 10.1021/jm0611152
22727351 19753 0 None -28 3 Human 5.8 pKi = 5.8 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 406 8 0 6 4.4 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1189537 19753 0 None -28 3 Human 5.8 pKi = 5.8 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 406 8 0 6 4.4 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL538977 19753 0 None -28 3 Human 5.8 pKi = 5.8 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 406 8 0 6 4.4 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
122442272 145126 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3769968 145126 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL3771384 145126 0 None -60 15 Human 5.8 pKi = 5.8 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 239 5 1 2 2.6 C=CCOc1cc(F)c(F)cc1C1CC1CN 10.1021/acs.jmedchem.5b01153
CHEMBL5288366 201199 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 433 5 1 3 4.6 Cc1c(Cl)cccc1NC(=O)CN1CCC2(CCCN2Cc2ccc(F)c(F)c2)C1 10.1016/j.ejmech.2022.114840
60167451 82123 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037520 82123 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
10456166 126411 0 None -691 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0611152
CHEMBL346692 126411 0 None -691 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0611152
CHEMBL4285942 126411 0 None -691 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm0611152
44339984 174576 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL430522 174576 0 None 10 4 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10641955 213627 0 None 154 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1cccc(Cl)c1)CC3 10.1021/jm970170v
CHEMBL90569 213627 0 None 154 3 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1cccc(Cl)c1)CC3 10.1021/jm970170v
44394820 71625 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 402 6 1 3 5.1 CSc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL182075 71625 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 402 6 1 3 5.1 CSc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
44394629 72349 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccc(F)c2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL183160 72349 0 None 234 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccc(F)c2)cc1 10.1016/j.bmcl.2004.07.045
44214764 73973 0 None 467 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 424 5 1 2 5.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL187804 73973 0 None 467 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 424 5 1 2 5.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.07.045
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00421-2
15522515 104937 0 None 93 4 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 292 3 0 4 2.7 c1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL273860 104937 0 None 93 4 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 292 3 0 4 2.7 c1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
10641955 213627 0 None 154 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1cccc(Cl)c1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL90569 213627 0 None 154 3 Human 7.8 pKi = 7.8 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1cccc(Cl)c1)CC3 10.1016/j.ejmech.2020.113034
44403232 77851 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 459 8 1 4 4.0 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
CHEMBL195247 77851 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 459 8 1 4 4.0 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
9949554 23625 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL124835 23625 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
44395741 188360 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL476935 188360 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL558392 188360 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
155567971 182800 0 None 25 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 495 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4589982 182800 0 None 25 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 495 9 2 4 4.9 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)01056-9
9861462 90109 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
CHEMBL219179 90109 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 3 2 5 2.0 Oc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)nc1 10.1021/jm060662k
52945819 24325 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 354 6 0 3 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1258037 24325 0 None -1 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 354 6 0 3 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2014.12.045
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human recombinant D4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401895u
137640391 163484 0 None -21 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4070091 163484 0 None -21 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
21219167 106429 0 None 93 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1c(-c2ccccc2)nnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL284346 106429 0 None 93 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1c(-c2ccccc2)nnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
10665598 41857 1 None 30 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4Cl)CC3)c2c1 10.1021/jm0009989
CHEMBL143355 41857 1 None 30 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4Cl)CC3)c2c1 10.1021/jm0009989
22100964 210734 4 None 93 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 324 3 0 3 4.8 Clc1ccc2oc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
CHEMBL69356 210734 4 None 93 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 324 3 0 3 4.8 Clc1ccc2oc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
44395741 188360 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL476935 188360 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL558392 188360 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44395741 188360 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476935 188360 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL558392 188360 0 None 1 10 Human 7.8 pKi = 7.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
44395741 188360 0 None -1 10 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL476935 188360 0 None -1 10 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
CHEMBL558392 188360 0 None -1 10 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2014.04.026
10015731 214948 0 None -15 4 Human 7.8 pKi = 7.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@H]21 10.1021/jm0000113
CHEMBL98305 214948 0 None -15 4 Human 7.8 pKi = 7.8 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@H]21 10.1021/jm0000113
127053217 146096 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792556 146096 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.1 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4c3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
11581443 103176 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to D4 receptorBinding affinity to D4 receptor
ChEMBL 367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL26188 103176 0 None -85 4 Human 6.8 pKi = 6.8 Binding
Binding affinity to D4 receptorBinding affinity to D4 receptor
ChEMBL 367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
9837137 119103 0 None 24 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 204 0 1 2 2.9 Cc1sc(C)c2c1CCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL329276 119103 0 None 24 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 204 0 1 2 2.9 Cc1sc(C)c2c1CCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
127031508 146159 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793169 146159 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
11624518 207122 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2012.08.011
CHEMBL597601 207122 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2012.08.011
145990453 173724 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 404 7 2 4 4.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc3ccccc3c1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4287062 173724 0 None -63 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 404 7 2 4 4.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc3ccccc3c1)CC2 10.1021/acsmedchemlett.8b00229
168290895 198778 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5201507 198778 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
168290895 198778 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5201507 198778 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.5 Cn1ncc2cc(CN3CCC(OCc4ccc(Cl)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
49783041 23943 0 None -42 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 597 7 1 3 6.8 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256171 23943 0 None -42 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 597 7 1 3 6.8 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
44436603 151994 0 None -7 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL391257 151994 0 None -7 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
44249745 202222 1 None -229 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
CHEMBL552373 202222 1 None -229 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
CHEMBL567286 202222 1 None -229 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
4420454 63033 6 None 1 5 Human 6.8 pKi = 6.8 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 63033 6 None 1 5 Human 6.8 pKi = 6.8 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
44304603 209917 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL64139 209917 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
44304621 210198 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL65641 210198 0 None -1 4 Human 6.8 pKi = 6.8 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
10276451 207064 37 None -776 9 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL2112910 207064 37 None -776 9 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL59725 207064 37 None -776 9 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
131801154 177030 0 None -14 3 Human 6.8 pKi = 6.8 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 432 7 1 5 4.0 Cn1ccc2c(N3CCN(CCCCOc4ccc5c(c4)NC(=O)CC5)CC3)cccc21 10.1021/acs.jmedchem.1c00704
CHEMBL4445841 177030 0 None -14 3 Human 6.8 pKi = 6.8 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 432 7 1 5 4.0 Cn1ccc2c(N3CCN(CCCCOc4ccc5c(c4)NC(=O)CC5)CC3)cccc21 10.1021/acs.jmedchem.1c00704
44437897 159832 0 None -77 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 352 6 1 3 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL397592 159832 0 None -77 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 352 6 1 3 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)ccc1OC 10.1016/j.bmc.2007.07.017
11615489 76218 1 None -3 4 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
CHEMBL193337 76218 1 None -3 4 Human 5.8 pKi = 5.8 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
11708363 78677 1 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL197159 78677 1 None -5 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL5288366 201199 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 433 5 1 3 4.6 Cc1c(Cl)cccc1NC(=O)CN1CCC2(CCCN2Cc2ccc(F)c(F)c2)C1 10.1016/j.ejmech.2022.114840
60167451 82123 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL2037520 82123 0 None -26 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
60167451 82123 0 None -26 7 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037520 82123 0 None -26 7 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 468 7 1 6 5.3 O=C(CCCCN1CCC(n2c(=O)[nH]c3cc(Cl)ccc32)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
44338248 15123 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 458 6 1 2 6.7 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cc3ccccc3[nH]2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL109299 15123 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 458 6 1 2 6.7 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2cc3ccccc3[nH]2)c2ccc(F)cc2)cc1 10.1021/jm010146o
155516494 176900 0 None 269 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443848 176900 0 None 269 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 358 5 1 4 3.1 CCc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10438027 72962 0 None -645 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
CHEMBL184383 72962 0 None -645 6 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
11408135 130966 0 None 6 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
CHEMBL363406 130966 0 None 6 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
168275089 197275 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5179198 197275 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.ejmech.2022.114840
168292951 198927 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5203807 198927 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
168292951 198927 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5203807 198927 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
168292951 198927 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5203807 198927 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
44582676 196558 0 None -1 17 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 196558 0 None -1 17 Human 6.8 pKi = 6.8 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
44393658 130873 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 475 7 1 3 5.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(C(c4ccccc4)c4ccccc4)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL363308 130873 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 475 7 1 3 5.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(C(c4ccccc4)c4ccccc4)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
168275089 197275 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5179198 197275 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)c1 10.1016/j.ejmech.2022.114840
118643968 152748 2 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
CHEMBL3918282 152748 2 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
118643968 152748 2 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01373
CHEMBL3918282 152748 2 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 498 10 1 4 4.0 [O-][S+](CCN1CCN(CC(O)Cc2ccccc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.6b01373
42626317 63026 0 None -346 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CCC(O)CNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627322 63026 0 None -346 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CCC(O)CNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
44350664 124927 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL340816 124927 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL553417 124927 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44350664 124927 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL340816 124927 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL553417 124927 0 None -1 6 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
9931571 12107 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 1 4 2.5 O=C(O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL106827 12107 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 1 4 2.5 O=C(O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL5086564 221814 0 None -316 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
71658204 97180 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 465 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386618 97180 0 None -37 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 465 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)s2)CC1 10.1016/j.bmc.2013.03.074
11351639 67298 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049465g
CHEMBL175734 67298 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049465g
11351639 67298 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL175734 67298 0 None -95 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
56593482 10713 3 None -162 9 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7650 10713 3 None -162 9 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165119 10713 3 None -162 9 Human 6.8 pKi = 6.8 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
3037308 50853 27 None -74 6 Human 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
CHEMBL151475 50853 27 None -74 6 Human 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
154727843 183212 1 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4448853 183212 1 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4596221 183212 1 None -1 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
44394590 134327 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL366304 134327 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
71458071 86275 0 None 43 6 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
CHEMBL2113718 86275 0 None 43 6 Human 7.8 pKi = 7.8 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
10735405 214190 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 333 4 1 4 4.1 Oc1nc(-c2ccccc2)cn1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL93958 214190 0 None 4 3 Human 7.8 pKi = 7.8 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 333 4 1 4 4.1 Oc1nc(-c2ccccc2)cn1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10947658 35475 0 None -16 16 Human 7.8 pKi = 7.8 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 35475 0 None -16 16 Human 7.8 pKi = 7.8 Binding
Binding affinity against Dopamine receptor D4Binding affinity against Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
44278789 106693 0 None 131 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 377 7 1 4 4.1 OC(COc1cccc2ccccc12)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL286177 106693 0 None 131 2 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 377 7 1 4 4.1 OC(COc1cccc2ccccc12)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
4088306 107414 6 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 1 3 4.0 OC(COc1ccc(Cl)cc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL29206 107414 6 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 1 3 4.0 OC(COc1ccc(Cl)cc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
135481864 19122 0 None 112 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1185415 19122 0 None 112 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL412665 19122 0 None 112 3 Human 7.8 pKi = 7.8 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 350 5 1 5 2.9 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
10837494 214233 0 None 38 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL94200 214233 0 None 38 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
155516873 176907 0 None 28 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 445 9 2 6 2.9 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4443944 176907 0 None 28 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 445 9 2 6 2.9 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm2013419
25072635 118560 0 None -8 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
CHEMBL3287399 118560 0 None -8 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
11720302 173037 0 None -9 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 503 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(F)c2F)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL426863 173037 0 None -9 5 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 503 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(F)c2F)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
21219156 102601 0 None 67 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1nnn(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL25887 102601 0 None 67 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 332 4 0 4 4.1 Cc1nnn(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
44376241 126893 0 None 51 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 354 5 0 6 2.5 COc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL351098 126893 0 None 51 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 354 5 0 6 2.5 COc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
135398737 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
38 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
722 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
CHEMBL42 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
DB00363 7745 93 None -13 90 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0104825
127032083 146225 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793996 146225 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 1 4 2.8 c1ccc(OC[C@@H]2CN(Cc3n[nH]c4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
9967004 46131 1 None 45 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2ccc(CN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm990277d
CHEMBL147130 46131 1 None 45 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2ccc(CN3CCN(c4ccccc4)CC3)cc2N1 10.1021/jm990277d
44591045 183516 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2008.12.054
CHEMBL460223 183516 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2008.12.054
11681599 81948 0 None -338 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 dopamine receptor by radioligand binding assayBinding affinity to D4 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 81948 0 None -338 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 dopamine receptor by radioligand binding assayBinding affinity to D4 dopamine receptor by radioligand binding assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
44380697 64867 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL167414 64867 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
11624518 207122 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL597601 207122 3 None -1 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 352 4 0 4 3.8 Clc1ccc(-n2cc(CN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
60165413 82135 0 None -52 7 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 378 7 0 4 5.5 O=C(CCCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037531 82135 0 None -52 7 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 378 7 0 4 5.5 O=C(CCCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
122189392 130025 0 None -81 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613878 130025 0 None -81 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
122177642 127988 0 None -81 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577343 127988 0 None -81 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
11348526 13133 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 7 0 4 3.5 CCOc1ccccc1OCC1CN(Cc2ccc(F)cc2)CCO1 10.1021/jm031111m
CHEMBL108211 13133 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 7 0 4 3.5 CCOc1ccccc1OCC1CN(Cc2ccc(F)cc2)CCO1 10.1021/jm031111m
10786474 213949 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 6 0 4 3.2 COc1cccc(C(=O)N(C)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL92411 213949 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 6 0 4 3.2 COc1cccc(C(=O)N(C)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
44371996 60397 0 None 2 4 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 500 6 0 6 4.6 Clc1ccc(N2CCN(Cc3cnn4c(N5CCN(Cc6ccccc6)CC5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL160266 60397 0 None 2 4 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 500 6 0 6 4.6 Clc1ccc(N2CCN(Cc3cnn4c(N5CCN(Cc6ccccc6)CC5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
11223708 173088 0 None 1 2 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL427173 173088 0 None 1 2 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
44263882 104000 0 None 2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4ccc5ccccc5c34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL268558 104000 0 None 2 3 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4ccc5ccccc5c34)CC2)cc1 10.1016/s0960-894x(98)00692-1
45482180 204683 0 None -218 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 544 12 1 7 4.6 COc1ccc(-n2cc(CCCC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
CHEMBL572867 204683 0 None -218 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 544 12 1 7 4.6 COc1ccc(-n2cc(CCCC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
25139478 191735 0 None -138 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
CHEMBL485384 191735 0 None -138 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
44319361 212499 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL82527 212499 0 None -1 4 Human 5.8 pKi = 5.8 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL5084145 221677 0 None -977 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCN1CCc2ccc(C#N)cc2C1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
21559988 120204 3 None -28 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 389 5 1 3 4.0 O=C(CCC(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.06.079
CHEMBL3318852 120204 3 None -28 4 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 389 5 1 3 4.0 O=C(CCC(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.06.079
168279082 197512 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5182602 197512 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
168279082 197512 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5182602 197512 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
44431485 94847 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 389 5 1 4 4.1 O=C(NC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234644 94847 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 389 5 1 4 4.1 O=C(NC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
44415569 172713 0 None -1148 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL425069 172713 0 None -1148 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
168279082 197512 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5182602 197512 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
51354275 66958 0 None -165 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 479 10 1 5 4.9 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1689012 66958 0 None -165 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 479 10 1 5 4.9 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1739787 66958 0 None -165 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 479 10 1 5 4.9 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
12280580 50843 2 None -2 3 Human 6.7 pKi = 6.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL15146 50843 2 None -2 3 Human 6.7 pKi = 6.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
71062889 155053 0 None 19 5 Mouse 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
CHEMBL3936595 155053 0 None 19 5 Mouse 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 5 0 5 1.8 O=C(CN1CCO[C@H](COc2cccnc2)C1)N1CCc2ccccc21 nan
10894276 48097 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 383 2 1 5 4.3 Cc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148965 48097 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 383 2 1 5 4.3 Cc1ccc2c(c1)C(N1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
168280464 197515 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
CHEMBL5182635 197515 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 335 5 0 4 3.8 Cc1ccccc1CO[C@H]1CCCN(Cc2cn3ccccc3n2)C1 10.1016/j.bmcl.2022.128615
154703764 183089 1 None -46 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 505 13 1 4 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4455719 183089 1 None -46 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 505 13 1 4 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595265 183089 1 None -46 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 505 13 1 4 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
71458739 88598 0 None -112 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2ccc3ccccc3c2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
CHEMBL2164347 88598 0 None -112 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2ccc3ccccc3c2)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
16090821 88608 0 None -47 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
CHEMBL216439 88608 0 None -47 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
53248673 73178 0 None -724 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 441 10 1 5 3.9 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1813591 73178 0 None -724 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 441 10 1 5 3.9 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2N1 10.1016/j.bmc.2011.04.021
CHEMBL1851831 73178 0 None -724 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 441 10 1 5 3.9 O=C1CCc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2N1 10.1016/j.bmc.2011.04.021
90644071 118819 0 None 1 5 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289655 118819 0 None 1 5 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
37461 23906 14 None -208 8 Human 6.7 pKi = 6.7 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1016/S0960-894X(97)00194-7
CHEMBL1255588 23906 14 None -208 8 Human 6.7 pKi = 6.7 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1016/S0960-894X(97)00194-7
10436285 108729 0 None -478 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL301242 108729 0 None -478 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
1599 9120 50 None -2238 16 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
3955 9120 50 None -2238 16 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
7215 9120 50 None -2238 16 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL841 9120 50 None -2238 16 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
DB00836 9120 50 None -2238 16 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10436285 108729 0 None -478 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
CHEMBL301242 108729 0 None -478 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 507 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm040190e
118719796 122501 0 None -102 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 456 9 0 7 4.4 COc1ccccc1N1CCN(CCCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353899 122501 0 None -102 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 456 9 0 7 4.4 COc1ccccc1N1CCN(CCCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
164608999 191163 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4845741 191163 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
71659909 97166 0 None -263 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccsc3)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386604 97166 0 None -263 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccsc3)cc2)CC1 10.1016/j.bmc.2013.03.074
168271806 197298 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
CHEMBL5179482 197298 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 353 5 0 4 4.0 Cc1cc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)ccc1F 10.1016/j.bmcl.2022.128615
44415690 86912 0 None -851 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213336 86912 0 None -851 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
164608999 191163 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4845741 191163 0 None -141 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 310 6 1 4 2.8 Nc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
135887931 18839 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 364 6 1 5 3.3 c1ccc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183657 18839 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 364 6 1 5 3.3 c1ccc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL309858 18839 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 364 6 1 5 3.3 c1ccc(N2CCN(CCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
122205437 144089 0 None -61 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
CHEMBL3752512 144089 0 None -61 5 Human 6.7 pKi = 6.7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
71658073 97174 0 None -24 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 401 8 1 5 3.8 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(C)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386612 97174 0 None -24 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 401 8 1 5 3.8 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(C)s2)CC1 10.1016/j.bmc.2013.03.074
72191067 99131 0 None -14 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 392 8 0 7 3.0 COc1ccccc1N1CCN(CCCCn2cc(-c3cccnc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430439 99131 0 None -14 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 392 8 0 7 3.0 COc1ccccc1N1CCN(CCCCn2cc(-c3cccnc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
10497179 211890 1 None 3 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 3 4.6 c1ccc(CCN2CCC(c3cc(-c4cccs4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL77743 211890 1 None 3 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 337 5 1 3 4.6 c1ccc(CCN2CCC(c3cc(-c4cccs4)[nH]n3)CC2)cc1 10.1021/jm970111h
135492584 18105 0 None 95 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179503 18105 0 None 95 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80645 18105 0 None 95 3 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 7 1 7 2.5 c1cnc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
44380715 65787 0 None 2 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL169222 65787 0 None 2 4 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
10639353 121574 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 319 3 0 3 4.2 O=c1ccc2ccc(CN3CCC(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL333983 121574 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 319 3 0 3 4.2 O=c1ccc2ccc(CN3CCC(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
155560295 181826 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 463 9 2 6 3.0 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4567758 181826 0 None 19 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 463 9 2 6 3.0 O=C(NCCCN1CCN(c2ncccn2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
10224165 175838 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 423 3 0 3 4.1 CC1(C)Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
CHEMBL439646 175838 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 423 3 0 3 4.1 CC1(C)Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
135398745 9688 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
47 9688 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
CHEMBL715 9688 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
DB00334 9688 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
52947756 23942 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 567 6 0 2 8.3 O=C(CCCN1CCC(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256170 23942 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 567 6 0 2 8.3 O=C(CCCN1CCC(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
11742798 103888 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 418 7 2 6 2.5 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL26758 103888 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 418 7 2 6 2.5 COc1cc(N)c(Cl)cc1C(=O)NCCN1CCN(c2ccccc2OC)CC1 10.1016/S0960-894X(97)00218-7
53364154 70617 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 31 0 16 9.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803025 70617 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1013 31 0 16 9.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53364227 70621 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 0 19 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803029 70621 0 None -3 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1033 32 0 19 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53363202 70630 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 961 28 0 15 8.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(C5CCCCC5)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803055 70630 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 961 28 0 15 8.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(C5CCCCC5)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
118709176 120201 0 None -13 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1106 29 0 14 11.8 O=C(CCc1cn(CCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318849 120201 0 None -13 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1106 29 0 14 11.8 O=C(CCc1cn(CCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137644833 164918 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4087187 164918 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
71459760 90847 0 None 3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 398 5 0 3 5.3 CCCC#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
CHEMBL2207634 90847 0 None 3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 398 5 0 3 5.3 CCCC#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
13091273 189217 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL478617 189217 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL553327 189217 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
127053219 146242 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794174 146242 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 335 5 0 3 3.8 Fc1cc(CN2CCO[C@H](COc3ccccc3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
13091273 189217 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL478617 189217 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL553327 189217 0 None -8 6 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL5083441 221638 0 None 9 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(c3cccc(O)c3)c3cccc(O)c3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
90644062 118811 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 118811 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
44372296 126265 0 None 72 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1021/jm0611152
CHEMBL345357 126265 0 None 72 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1021/jm0611152
10690882 204313 0 None 501 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 6 0 4 4.5 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
CHEMBL57019 204313 0 None 501 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 6 0 4 4.5 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
10548329 209407 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL61248 209407 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
44273741 85282 0 None 31 2 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 429 7 1 3 4.6 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
CHEMBL21119 85282 0 None 31 2 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 429 7 1 3 4.6 O=C(NCCCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
137644962 165272 0 None 74 8 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4091058 165272 0 None 74 8 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 363 6 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
135398745 9688 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
47 9688 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
CHEMBL715 9688 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
DB00334 9688 112 None -10 65 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm070516u
11779642 213638 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL90654 213638 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
25139479 191096 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
CHEMBL484202 191096 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
57390119 76078 0 None -45 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928127 76078 0 None -45 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
137655556 165318 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4091507 165318 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
44436610 98724 0 None -25 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
CHEMBL241436 98724 0 None -25 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
52937777 67945 0 None -323 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 464 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(Cl)c2C1 10.1021/jm101639t
CHEMBL1765630 67945 0 None -323 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 464 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(Cl)c2C1 10.1021/jm101639t
CHEMBL5289063 201234 0 None -56 2 Human 6.7 pKi = 6.7 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccc5ccnn5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.1c00704
155562543 181951 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4570411 181951 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
10667966 63934 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 387 5 0 1 6.1 CCCN(CCC)C1CCC(=C(C#C[Si](C)(C)C)C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL164736 63934 0 None 1 4 Human 5.7 pKi = 5.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 387 5 0 1 6.1 CCCN(CCC)C1CCC(=C(C#C[Si](C)(C)C)C#C[Si](C)(C)C)CC1 10.1021/jm991098z
42626240 63011 0 None -239 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
CHEMBL1627307 63011 0 None -239 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
11626748 146937 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 459 4 0 7 3.1 CN1CCN(c2ccc3nc(CN4CCN(c5ccc(Cl)c(Cl)c5)CC4)cn3n2)CC1 10.1021/jm060166w
CHEMBL380287 146937 0 None -2 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 459 4 0 7 3.1 CN1CCN(c2ccc3nc(CN4CCN(c5ccc(Cl)c(Cl)c5)CC4)cn3n2)CC1 10.1021/jm060166w
155562543 181951 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4570411 181951 0 None -3 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 353 4 0 4 3.2 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccccn2)CC1 10.1016/j.bmc.2020.115943
22910005 18371 1 None -147 5 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)OC(CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL1180629 18371 1 None -147 5 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)OC(CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL135395 18371 1 None -147 5 Human 6.7 pKi = 6.7 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)OC(CNCc1ccccc1)CC2 10.1021/jm9703653
25141535 63012 0 None -1380 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627308 63012 0 None -1380 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 422 8 3 5 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
10515841 215044 0 None -54 3 Human 6.7 pKi = 6.7 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@@H]21 10.1021/jm0000113
CHEMBL98836 215044 0 None -54 3 Human 6.7 pKi = 6.7 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCO[C@@H]2c3cc(O)ccc3SC[C@@H]21 10.1021/jm0000113
71062567 167194 0 None -2 2 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccnc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4111349 167194 0 None -2 2 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccnc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
168280776 197937 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5188602 197937 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 339 5 0 4 3.7 Fc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
134136246 149316 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3890841 149316 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
134136246 149316 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
CHEMBL3890841 149316 0 None -2 6 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 275 3 0 1 4.1 C1=C(CCN2CCc3ccccc3C2)Cc2ccccc21 10.1016/j.bmc.2016.09.019
44438227 100330 0 None -18 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.3 OCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246437 100330 0 None -18 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.3 OCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
25130157 110084 0 None -275 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
CHEMBL3084515 110084 0 None -275 6 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
130431303 179716 0 None -173 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 419 8 3 5 2.2 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4516799 179716 0 None -173 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 419 8 3 5 2.2 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
3246443 44460 2 None -316 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL1457510 44460 2 None -316 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
1353 8692 93 None -3 85 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 8692 93 None -3 85 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 8692 93 None -3 85 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 8692 93 None -3 85 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 8692 93 None -3 85 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
22727335 20257 0 None -20 3 Human 6.7 pKi = 6.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 391 8 0 5 4.5 COc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1193307 20257 0 None -20 3 Human 6.7 pKi = 6.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 391 8 0 5 4.5 COc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL544689 20257 0 None -20 3 Human 6.7 pKi = 6.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 391 8 0 5 4.5 COc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
168280974 197642 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5184607 197642 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 361 6 0 3 4.5 COc1ccc(CN2CCC[C@@H](OCc3ccc(F)c(C)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
10524285 209200 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.3 COc1cc2ccccc2cc1CC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL61090 209200 0 None 6 2 Human 6.7 pKi = 6.7 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.3 COc1cc2ccccc2cc1CC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
42273483 172074 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 5 1 3 3.0 CC(C)(C)C(=O)NCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL423287 172074 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 5 1 3 3.0 CC(C)(C)C(=O)NCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
75306277 116031 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 116031 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D4 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
168275381 197049 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5175548 197049 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
11384664 89887 0 None -234 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm0611152
CHEMBL218203 89887 0 None -234 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 7 1 3 4.8 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm0611152
153287574 182026 0 None -26 10 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4572167 182026 0 None -26 10 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-methylspiperone from human recombinant dopamine D4 receptor expressed in Stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 266 2 1 2 4.0 CC[C@H]1c2ccccc2N(c2ccccc2)C[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
10245409 56563 0 None 99 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL156732 56563 0 None 99 3 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 319 5 1 2 4.4 c1ccc(CCC2CCN(Cc3cc4ccc[nH]c-4n3)CC2)cc1 10.1016/s0960-894x(99)00025-6
44214767 73816 0 None 602 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL187122 73816 0 None 602 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
44394666 132570 0 None 501 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL364782 132570 0 None 501 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2ccsc2)cc1 10.1016/j.bmcl.2004.07.045
44394742 172900 0 None 34 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL426062 172900 0 None 34 2 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
210956 213523 6 None 3 3 Human 8.7 pKi = 8.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL89970 213523 6 None 3 3 Human 8.7 pKi = 8.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
10570080 113911 0 None 41 3 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CC2CCCCC2)CC1 10.1021/jm991029k
CHEMBL316125 113911 0 None 41 3 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 353 4 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CC2CCCCC2)CC1 10.1021/jm991029k
210956 213523 6 None 3 3 Human 8.7 pKi = 8.7 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL89970 213523 6 None 3 3 Human 8.7 pKi = 8.7 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 292 1 0 3 3.5 CN1CCN(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00043a008
9840365 115229 0 None 109 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL31991 115229 0 None 109 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 O[C@@H](COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10404144 212081 23 None 1 10 Human 8.7 pKi = 8.7 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7927 212081 23 None 1 10 Human 8.7 pKi = 8.7 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44336061 115398 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/j.ejmech.2020.113141
CHEMBL320597 115398 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/j.ejmech.2020.113141
792265 98929 8 None 29 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 346 5 0 3 4.6 CCOc1ccccc1N1CCN(Cc2cccc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420781 98929 8 None 29 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 346 5 0 3 4.6 CCOc1ccccc1N1CCN(Cc2cccc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
9860183 114006 0 None 89 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL316727 114006 0 None 89 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
10588194 25692 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128524 25692 3 None 67 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 271 9 1 3 3.1 c1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
44336061 115398 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL320597 115398 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
44335889 114131 0 None 354 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 381 4 0 3 3.2 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1F 10.1016/s0960-894x(02)00656-x
CHEMBL317670 114131 0 None 354 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 381 4 0 3 3.2 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1F 10.1016/s0960-894x(02)00656-x
44336074 11666 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 393 5 0 4 4.2 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104497 11666 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 393 5 0 4 4.2 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/s0960-894x(02)00655-8
44335812 11710 0 None 19 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL104716 11710 0 None 19 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44336074 11666 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 393 5 0 4 4.2 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.ejmech.2020.113141
CHEMBL104497 11666 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 393 5 0 4 4.2 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc([N+](=O)[O-])cc2)CC1 10.1016/j.ejmech.2020.113141
11464857 11553 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 439 6 0 4 4.8 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Br)cc2)CCCO1 10.1016/j.ejmech.2020.113141
CHEMBL104035 11553 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 439 6 0 4 4.8 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Br)cc2)CCCO1 10.1016/j.ejmech.2020.113141
137659990 166009 0 None -3 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 166009 0 None -3 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
122180955 128548 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 386 7 1 3 4.6 CCCN(CCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589576 128548 0 None 1 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 386 7 1 3 4.6 CCCN(CCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
11559581 85193 0 None 194 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 3 0 5 3.4 Clc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL211135 85193 0 None 194 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 361 3 0 5 3.4 Clc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
10476504 40261 1 None -1 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL142020 40261 1 None -1 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
11464857 11553 0 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 4.8 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Br)cc2)CCCO1 10.1021/jm031111m
CHEMBL104035 11553 0 None - 1 Human 8.7 pKi = 8.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 4.8 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Br)cc2)CCCO1 10.1021/jm031111m
44376209 63106 0 None 33 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL163009 63106 0 None 33 2 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@H]2CC[C@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44336061 115398 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL320597 115398 0 None 56 2 Human 8.7 pKi = 8.7 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1021/acs.jmedchem.7b00151
119570 9933 96 None -6 39 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 9933 96 None -6 39 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 9933 96 None -6 39 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 9933 96 None -6 39 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 9933 96 None -6 39 Human 8.7 pKi = 8.7 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
10571927 214193 0 None - 1 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2Cl)CC1 10.1021/jm991029k
CHEMBL93970 214193 0 None - 1 Human 8.7 pKi = 8.7 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2ccccc2)nc(O)n1C1CCN(Cc2ccccc2Cl)CC1 10.1021/jm991029k
1353 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
3559 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
86 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
CHEMBL54 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
DB00502 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
9802631 118774 1 None 104 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL328866 118774 1 None 104 4 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
10716980 214616 0 None 39 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 419 6 2 4 3.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCC2)C1 10.1021/jm9601720
CHEMBL96369 214616 0 None 39 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 419 6 2 4 3.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCC2)C1 10.1021/jm9601720
18624462 173722 0 None 10 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4Binding affinity towards human Dopamine receptor D4
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm030480f
CHEMBL428705 173722 0 None 10 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4Binding affinity towards human Dopamine receptor D4
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm030480f
10831735 38529 0 None 2511 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140594 38529 0 None 2511 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)cc4)CC3)cc2c1 10.1021/jm0009989
137655636 165515 0 None 93 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4093527 165515 0 None 93 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 376 7 0 2 4.7 O=C1CCc2ccccc2N1CCCN1CCC(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
10336538 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0611152
974 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0611152
CHEMBL310843 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0611152
1353 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
3559 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
86 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
CHEMBL54 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
DB00502 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970170v
10336538 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
974 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
CHEMBL310843 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
10336538 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm049612a
974 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm049612a
CHEMBL310843 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm049612a
10784211 110959 0 None 223 3 Rat 8.7 pKi = 8.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL309730 110959 0 None 223 3 Rat 8.7 pKi = 8.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
10336538 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
974 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
CHEMBL310843 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
1353 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
3559 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
86 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
CHEMBL54 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
DB00502 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970422s
778880 57121 11 None 26 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 339 6 1 4 2.2 COc1cccc(C(=O)NCCN2CCN(c3ccccc3)CC2)c1 10.1021/jm020952a
CHEMBL157222 57121 11 None 26 2 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 339 6 1 4 2.2 COc1cccc(C(=O)NCCN2CCN(c3ccccc3)CC2)c1 10.1021/jm020952a
1353 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
3559 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
86 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
CHEMBL54 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
DB00502 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00073a021
127032384 146154 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793137 146154 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
10336538 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.ejmech.2020.113141
974 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.ejmech.2020.113141
CHEMBL310843 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.ejmech.2020.113141
137643309 165194 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4090208 165194 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
10336538 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
974 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
CHEMBL310843 8406 50 None -3 8 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
1353 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
3559 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
86 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
CHEMBL54 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
DB00502 8692 93 None -3 85 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0104825
45361874 176800 2 None 48 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 176800 2 None 48 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
3303 9024 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
5311200 9024 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
CHEMBL267014 9024 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.2c00840
168285560 199697 0 None 1148 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5196873 199697 0 None 1148 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222201 199697 0 None 1148 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 350 5 0 4 2.6 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccn2)CC1 10.1021/acs.jmedchem.2c00840
3303 9024 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
5311200 9024 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
CHEMBL267014 9024 46 None 1 15 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1021/acs.jmedchem.8b00265
10404144 212081 23 None 1 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm0611152
CHEMBL7927 212081 23 None 1 10 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm0611152
1353 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
3559 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
86 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
CHEMBL54 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
DB00502 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm970111h
9847013 52134 0 None 26 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 458 6 1 5 6.3 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(NC2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL15270 52134 0 None 26 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 458 6 1 5 6.3 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(NC2CCN(Cc3ccccc3)CC2)n1 10.1016/s0960-894x(01)00167-6
1353 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
3559 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
86 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
CHEMBL54 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
DB00502 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9600712
11811808 52191 0 None -5 3 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 417 8 1 4 4.2 COc1cccc(C(=O)NCCCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL152756 52191 0 None -5 3 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 417 8 1 4 4.2 COc1cccc(C(=O)NCCCCN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/jm020952a
3645619 9808 20 None -5 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/acs.jmedchem.9b01085
975 9808 20 None -5 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/acs.jmedchem.9b01085
CHEMBL45244 9808 20 None -5 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/acs.jmedchem.9b01085
27620 147596 13 None 5 8 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818994 147596 13 None 5 8 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 297 5 0 2 3.8 O=C(CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
46893146 68381 0 None -19 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771110 68381 0 None -19 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
137634397 162884 0 None -8 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4063145 162884 0 None -8 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
1353 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
3559 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
86 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
CHEMBL54 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
DB00502 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960072u
11633170 85187 0 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 421 5 0 7 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(N4CCOCC4)c3n2)CC1 10.1021/jm060166w
CHEMBL211118 85187 0 None 63 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 421 5 0 7 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(N4CCOCC4)c3n2)CC1 10.1021/jm060166w
45273045 203155 0 None 199 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL562620 203155 0 None 199 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm900690y
10361512 61213 0 None 1949 5 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160932 61213 0 None 1949 5 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
10267394 107165 3 None 102 4 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28997 107165 3 None 102 4 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
1353 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
3559 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
86 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
CHEMBL54 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
DB00502 8692 93 None -3 85 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b00151
10042972 113317 0 None 131 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 341 2 1 4 3.7 O=c1oc2cc(O)ccc2c2c1CN(Cc1ccc(Cl)cc1)CC2 10.1021/jm970170v
CHEMBL314095 113317 0 None 131 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 341 2 1 4 3.7 O=c1oc2cc(O)ccc2c2c1CN(Cc1ccc(Cl)cc1)CC2 10.1021/jm970170v
10042972 113317 0 None 131 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 341 2 1 4 3.7 O=c1oc2cc(O)ccc2c2c1CN(Cc1ccc(Cl)cc1)CC2 10.1016/j.ejmech.2020.113034
CHEMBL314095 113317 0 None 131 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 341 2 1 4 3.7 O=c1oc2cc(O)ccc2c2c1CN(Cc1ccc(Cl)cc1)CC2 10.1016/j.ejmech.2020.113034
21533446 76930 0 None -6 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940403 76930 0 None -6 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
21527771 76931 1 None -1 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
CHEMBL1940404 76931 1 None -1 10 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
71463207 90849 0 None 7 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 357 4 0 4 4.0 COc1ccccc1N1CCN(Cc2cc(C#N)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207636 90849 0 None 7 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 357 4 0 4 4.0 COc1ccccc1N1CCN(Cc2cc(C#N)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
135524323 202205 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 382 5 2 6 1.6 COc1ccccc1N1CCN(Cc2cc3c(=O)[nH]c(N(C)C)nc3[nH]2)CC1 10.1016/j.bmc.2009.05.015
CHEMBL552268 202205 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 382 5 2 6 1.6 COc1ccccc1N1CCN(Cc2cc3c(=O)[nH]c(N(C)C)nc3[nH]2)CC1 10.1016/j.bmc.2009.05.015
9863333 211144 0 None -1 9 Human 8.6 pKi = 8.6 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm980137o
CHEMBL71724 211144 0 None -1 9 Human 8.6 pKi = 8.6 Binding
The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm980137o
44340333 16434 0 None 19 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL112833 16434 0 None 19 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
5029739 107603 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
CHEMBL293341 107603 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
13869641 120180 0 None -1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 431 8 0 4 5.4 CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318824 120180 0 None -1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 431 8 0 4 5.4 CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
9949442 102359 0 None 56 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL25772 102359 0 None 56 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 0 3 4.7 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00169-9
5029739 107603 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm960072u
CHEMBL293341 107603 1 None 190 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Cc1c(-c2ccc(Cl)cc2)noc1C1CCN(CCc2ccccc2)CC1 10.1021/jm960072u
71583848 94506 0 None 6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336892 94506 0 None 6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
133008 9022 22 None 204 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.7b00151
3302 9022 22 None 204 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.7b00151
CHEMBL444309 9022 22 None 204 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.7b00151
44412468 172709 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL425057 172709 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1021/jm0611152
10640530 119066 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 3 0 4 3.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C)cc1)CC3 10.1021/jm970170v
CHEMBL329126 119066 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 3 0 4 3.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C)cc1)CC3 10.1021/jm970170v
44323962 213609 0 None 7 4 Human 8.6 pKi = 8.6 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 369 3 1 2 4.3 Brc1ccc(N2CCN(Cc3ccccc3)CC2)c2cc[nH]c12 10.1016/s0960-894x(98)00474-0
CHEMBL90476 213609 0 None 7 4 Human 8.6 pKi = 8.6 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 369 3 1 2 4.3 Brc1ccc(N2CCN(Cc3ccccc3)CC2)c2cc[nH]c12 10.1016/s0960-894x(98)00474-0
10807795 46044 0 None 239 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
CHEMBL147059 46044 0 None 239 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 350 3 1 3 4.0 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
10664621 50736 0 None 91 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL151286 50736 0 None 91 3 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
76320592 92661 0 None 9 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 365 3 1 0 3.5 Brc1ccc(-[n+]2cc[n+](Cc3ccccc3)cc2)c2cc[nH]c12 10.1007/s00044-012-0055-5
CHEMBL2298809 92661 0 None 9 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 365 3 1 0 3.5 Brc1ccc(-[n+]2cc[n+](Cc3ccccc3)cc2)c2cc[nH]c12 10.1007/s00044-012-0055-5
10404144 212081 23 None -1 10 Rat 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D4 receptor in Wistar rat brain slicesBinding affinity to dopamine D4 receptor in Wistar rat brain slices
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm200762g
CHEMBL7927 212081 23 None -1 10 Rat 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D4 receptor in Wistar rat brain slicesBinding affinity to dopamine D4 receptor in Wistar rat brain slices
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm200762g
10640530 119066 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 335 3 0 4 3.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL329126 119066 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 335 3 0 4 3.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C)cc1)CC3 10.1016/j.ejmech.2020.113034
155510756 176291 0 None 10 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccccc2F)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4434714 176291 0 None 10 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccccc2F)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
155564308 181932 0 None 12 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 525 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4570073 181932 0 None 12 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 525 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
44412468 172709 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL425057 172709 0 None 61 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
44371932 126426 0 None 467 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 354 4 0 5 3.1 O=Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL346805 126426 0 None 467 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 354 4 0 5 3.1 O=Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
168268770 199551 0 None 213 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 5 0 3 3.7 c1ccc(N2CCN(CCCN3CCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5169993 199551 0 None 213 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 5 0 3 3.7 c1ccc(N2CCN(CCCN3CCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221238 199551 0 None 213 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 5 0 3 3.7 c1ccc(N2CCN(CCCN3CCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
49788870 25030 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 341 5 1 3 2.7 Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
CHEMBL1270322 25030 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 341 5 1 3 2.7 Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
10589218 27982 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL131299 27982 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
44270558 172067 0 None 812 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
CHEMBL423247 172067 0 None 812 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1021/jm0611152
44339992 115961 0 None 22 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL321492 115961 0 None 22 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10336538 8406 50 None -3 8 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
974 8406 50 None -3 8 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
CHEMBL310843 8406 50 None -3 8 Human 8.6 pKi = 8.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm0305669
10646459 213911 0 None 7 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 6 2 4 4.2 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCCC2)C1 10.1021/jm9601720
CHEMBL92199 213911 0 None 7 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 6 2 4 4.2 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2CCCCCC2)C1 10.1021/jm9601720
10589218 27982 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL131299 27982 0 None 23 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccc(OCCCNCCOc2ccccc2)cc1 10.1021/jm970422s
11724450 130626 4 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL184158 130626 4 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL362542 130626 4 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-spiperone from human D4 receptor assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
44412269 84875 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL210232 84875 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
44412269 84875 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210232 84875 0 None 33 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2006.02.075
11724450 130626 4 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL184158 130626 4 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL362542 130626 4 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.bmcl.2004.07.068
44270558 172067 0 None 812 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL423247 172067 0 None 812 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
119570 9933 96 None -6 39 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 9933 96 None -6 39 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 9933 96 None -6 39 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 9933 96 None -6 39 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 9933 96 None -6 39 Human 8.6 pKi = 8.6 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
6469693 86730 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1016/j.ejmech.2019.111569
CHEMBL212631 86730 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1016/j.ejmech.2019.111569
10854370 126384 0 None 18 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL346398 126384 0 None 18 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 336 3 1 3 3.7 Cc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
18403576 12963 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1016/j.ejmech.2020.113141
CHEMBL108122 12963 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1016/j.ejmech.2020.113141
54583897 68376 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 7 0 4 3.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(F)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771106 68376 0 None -1 5 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 7 0 4 3.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(F)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
6469693 86730 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 86730 17 None 158 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
44241718 202043 0 None 70 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 4 1 7 1.6 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccn4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL551199 202043 0 None 70 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 4 1 7 1.6 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccn4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
10249308 11675 0 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104550 11675 0 None - 1 Human 8.6 pKi = 8.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
15512070 60016 0 None 426 2 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 342 4 0 5 2.6 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL159903 60016 0 None 426 2 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 342 4 0 5 2.6 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44372338 60620 0 None 707 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 398 4 0 4 3.9 C[Si](C)(C)c1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160454 60620 0 None 707 4 Human 8.6 pKi = 8.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 398 4 0 4 3.9 C[Si](C)(C)c1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
44278115 108296 0 None 181 3 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 318 4 1 3 3.5 C=Cc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL29808 108296 0 None 181 3 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 318 4 1 3 3.5 C=Cc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
137649896 164312 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.7b00151
CHEMBL4080034 164312 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.7b00151
137649896 164312 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.8b00265
CHEMBL4080034 164312 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 381 6 0 4 4.3 COc1ccc(Cl)cc1OC[C@@H]1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/acs.jmedchem.8b00265
14925759 164817 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL4085780 164817 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
14925759 164817 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4085780 164817 6 None 18 13 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 349 5 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
44412494 85096 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL210955 85096 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
17475863 175563 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
CHEMBL437490 175563 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1021/jm0611152
44323763 213272 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
CHEMBL88289 213272 0 None -2 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1nc2c(N3CCN(Cc4ccccc4)CC3)cccc2[nH]1 10.1016/s0960-894x(98)00474-0
76309673 92664 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 356 3 1 1 3.2 FC(F)(F)c1nc2c(-[n+]3cc[n+](Cc4ccccc4)cc3)cccc2[nH]1 10.1007/s00044-012-0055-5
CHEMBL2298812 92664 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 356 3 1 1 3.2 FC(F)(F)c1nc2c(-[n+]3cc[n+](Cc4ccccc4)cc3)cccc2[nH]1 10.1007/s00044-012-0055-5
60785 212672 48 None -23 7 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm0002432
CHEMBL83894 212672 48 None -23 7 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1021/jm0002432
155534246 178710 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 10 2 5 4.8 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4470231 178710 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 10 2 5 4.8 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.9b01085
155566058 182479 0 None 45 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccc(F)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4582096 182479 0 None 45 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2ccc(F)cc2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
54581964 68382 0 None -10 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 489 8 0 5 5.4 COc1ccccc1N1CCN(CCCCN2CCCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771111 68382 0 None -10 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 489 8 0 5 5.4 COc1ccccc1N1CCN(CCCCN2CCCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
60785 212672 48 None -23 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.051
CHEMBL83894 212672 48 None -23 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 425 5 0 4 3.7 O=S1(=O)c2cccc3cccc(c23)N1CCCN1CCN(c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.08.051
44412494 85096 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210955 85096 0 None 131 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
17475863 175563 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL437490 175563 3 None 41 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
11372852 11900 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105696 11900 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
49788942 25061 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 362 5 1 4 2.4 O=C(NCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1021/jm100925m
CHEMBL1270516 25061 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 362 5 1 4 2.4 O=C(NCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1021/jm100925m
10691523 112387 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4Cl)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL312255 112387 0 None 34 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4Cl)CC3)[nH]n2)cc1 10.1021/jm970111h
10837493 213883 0 None 37 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL92030 213883 0 None 37 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 455 7 2 4 4.5 COc1cc(NC(=O)C2CCCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
155547128 180440 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 399 7 1 5 3.8 COc1ccccc1N1CCN(CCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4534703 180440 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 399 7 1 5 3.8 COc1ccccc1N1CCN(CCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
90644062 118811 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 118811 0 None 8 5 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
49782600 24225 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 1 3 4.4 Cc1ccc(C)c(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1257689 24225 0 None -4 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 6 1 3 4.4 Cc1ccc(C)c(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
10548329 209407 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL61248 209407 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 388 6 1 3 4.5 COc1cc2ccccc2cc1C(=O)NCC1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
72544566 99906 0 None 5 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443009 99906 0 None 5 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
25333445 84898 5 None 104 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3ccc(-n4cccn4)cc3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210318 84898 5 None 104 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3ccc(-n4cccn4)cc3)CC2)cc1 10.1016/j.bmcl.2006.02.075
122191605 130498 0 None 2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622097 130498 0 None 2 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
44376230 126765 0 None 87 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 380 4 0 5 3.8 CC(C)(C)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL349904 126765 0 None 87 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 380 4 0 5 3.8 CC(C)(C)c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44372296 126265 0 None 72 4 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1016/s0960-894x(01)00814-9
CHEMBL345357 126265 0 None 72 4 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1016/s0960-894x(01)00814-9
71450812 85197 0 None 4 4 Human 7.7 pKi = 7.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111525 85197 0 None 4 4 Human 7.7 pKi = 7.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
11849776 86547 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
CHEMBL211836 86547 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 6 0 6 2.5 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C#N)c1 10.1021/jm060279f
667675 211911 3 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77969 211911 3 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
9820085 148108 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 Cc1nc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)sc1C 10.1016/s0960-894x(98)00252-2
CHEMBL38349 148108 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 356 4 1 5 2.8 Cc1nc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)sc1C 10.1016/s0960-894x(98)00252-2
44340186 16432 0 None 8 4 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
CHEMBL112831 16432 0 None 8 4 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
44380770 172491 0 None -6 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL424575 172491 0 None -6 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
3156990 14902 22 None 7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL109173 14902 22 None 7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
76441180 122515 0 None -95 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 437 9 0 7 4.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353913 122515 0 None -95 4 Human 6.7 pKi = 6.7 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 437 9 0 7 4.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
11658914 77015 1 None -30 3 Human 6.7 pKi = 6.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
CHEMBL194099 77015 1 None -30 3 Human 6.7 pKi = 6.7 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
11405182 115311 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 343 5 0 3 4.3 COc1ccccc1/C=C/C1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL320071 115311 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 343 5 0 3 4.3 COc1ccccc1/C=C/C1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
56597938 10712 3 None -204 9 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7651 10712 3 None -204 9 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165126 10712 3 None -204 9 Human 6.7 pKi = 6.7 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
168275381 197049 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5175548 197049 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
44415672 86949 0 None -1659 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213492 86949 0 None -1659 6 Human 5.7 pKi = 5.7 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
42605994 24646 0 None 8 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259071 24646 0 None 8 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
9865384 180274 35 None -2344 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
CHEMBL45305 180274 35 None -2344 7 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
56658008 73194 0 None -52 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 421 9 1 5 3.9 COc1ccccc1N1CCN(CCCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813599 73194 0 None -52 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 421 9 1 5 3.9 COc1ccccc1N1CCN(CCCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851895 73194 0 None -52 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 421 9 1 5 3.9 COc1ccccc1N1CCN(CCCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
10572229 127795 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 386 4 1 4 3.4 O=C1NCN(c2ccccc2)C12CCN(Cc1ccn(-c3ccccc3)c1)CC2 10.1021/jm00025a013
CHEMBL356542 127795 0 None -5 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 386 4 1 4 3.4 O=C1NCN(c2ccccc2)C12CCN(Cc1ccn(-c3ccccc3)c1)CC2 10.1021/jm00025a013
168275381 197049 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5175548 197049 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1ncc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
154725766 183424 1 None -1659 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4527244 183424 1 None -1659 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4598000 183424 1 None -1659 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL5094044 222243 2 None -30 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10737150 114313 0 None 2 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 358 7 0 3 4.5 COc1cccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL318747 114313 0 None 2 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 358 7 0 3 4.5 COc1cccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
168294958 199183 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5207898 199183 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
127051844 147625 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 147625 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
42626172 63018 0 None -1949 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 490 8 3 5 3.8 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm501512b
CHEMBL1627314 63018 0 None -1949 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 490 8 3 5 3.8 COc1ccc2[nH]c(C(=O)NCCC(O)CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2c1 10.1021/jm501512b
162659314 190475 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4762416 190475 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803145 190475 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
127051844 147625 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819427 147625 0 None -16 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 322 6 1 3 2.8 NC(=O)c1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
168294958 199183 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5207898 199183 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.bmcl.2022.128615
11771801 86804 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL212891 86804 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 328 5 0 5 2.4 CO/N=C(\CN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
162659314 190475 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4762416 190475 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803145 190475 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccncc3)CC2)cc1 10.1016/j.bmc.2020.115943
22953120 115246 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
CHEMBL319927 115246 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
168294958 199183 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5207898 199183 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 347 6 0 3 4.2 COc1ccc(CN2CCC[C@H](OCc3cccc(F)c3)C2)cc1F 10.1016/j.ejmech.2022.114840
1212 8443 50 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -77 65 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
168285068 198362 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5195130 198362 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.bmcl.2022.128615
154705038 183425 1 None -63 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4584481 183425 1 None -63 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4598001 183425 1 None -63 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
168285068 198362 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5195130 198362 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 0 4 4.5 FC(F)(F)c1cccc(COC2CCN(Cc3ncc4ccccn34)CC2)c1 10.1016/j.ejmech.2022.114840
168289523 198278 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5193761 198278 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.ejmech.2022.114840
127051845 147507 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 147507 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
10551026 108394 0 None 1 5 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL298875 108394 0 None 1 5 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44301054 202927 0 None 21 6 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL56118 202927 0 None 21 6 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
135398737 7745 93 None -13 90 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
38 7745 93 None -13 90 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
722 7745 93 None -13 90 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
CHEMBL42 7745 93 None -13 90 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
DB00363 7745 93 None -13 90 Human 7.7 pKi = 7.7 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00004a016
135398737 7745 93 None -13 90 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
38 7745 93 None -13 90 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
722 7745 93 None -13 90 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
CHEMBL42 7745 93 None -13 90 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
DB00363 7745 93 None -13 90 Human 7.7 pKi = 7.7 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
135418440 18840 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1183663 18840 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL310311 18840 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 351 5 1 6 2.3 c1ccc(N2CCN(CCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
3802 209802 21 None 1 5 Rat 7.7 pKi = 7.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm960084f
CHEMBL63329 209802 21 None 1 5 Rat 7.7 pKi = 7.7 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm960084f
21830793 98610 10 None -138 46 Human 7.7 pKi = 7.7 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 98610 10 None -138 46 Human 7.7 pKi = 7.7 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
9930934 115414 0 None 52 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 401 5 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CF 10.1016/s0960-894x(02)00656-x
CHEMBL320721 115414 0 None 52 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 401 5 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2C[C@H]1CF 10.1016/s0960-894x(02)00656-x
44336109 117727 0 None 24 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 400 4 0 2 5.1 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2Cl)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL326202 117727 0 None 24 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 400 4 0 2 5.1 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2Cl)CC1 10.1016/s0960-894x(02)00655-8
2435 10362 83 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
60149 10362 83 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
98 10362 83 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
CHEMBL12713 10362 83 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
DB06144 10362 83 None -10 48 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
9905246 23110 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 6 2 4 3.6 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1C 10.1021/jm990266k
CHEMBL122862 23110 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 6 2 4 3.6 Cc1ccc(NCCNCc2ccc3ccc(=O)oc3c2)cc1C 10.1021/jm990266k
155563950 182052 0 None 32 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 9 2 4 4.7 O=C(NCCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4572646 182052 0 None 32 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 9 2 4 4.7 O=C(NCCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
127028181 146227 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794013 146227 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 359 5 1 4 3.1 Fc1ccc2c(CN3CCO[C@H](COc4cccc(F)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
57391216 76943 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940416 76943 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57391216 76943 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940416 76943 0 None 1 8 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
44431490 95047 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL234826 95047 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
44405490 140228 0 None 35 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL370652 140228 0 None 35 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2ccc(C(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
137659303 166083 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4099711 166083 0 None -3 5 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
22100932 210874 0 None 31 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 374 3 0 3 5.9 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL70215 210874 0 None 31 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 374 3 0 3 5.9 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4s3)CC2)cc1 10.1016/S0960-894X(97)00402-2
45273442 203230 0 None 61 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 403 3 0 5 4.3 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL563078 203230 0 None 61 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 403 3 0 5 4.3 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
44276075 19997 0 None -4 3 Human 7.7 pKi = 7.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 397 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1191252 19997 0 None -4 3 Human 7.7 pKi = 7.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 397 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL542325 19997 0 None -4 3 Human 7.7 pKi = 7.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 397 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
10715225 213897 0 None 1 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 386 8 0 4 4.5 COc1cccc(C(=O)CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL92121 213897 0 None 1 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 386 8 0 4 4.5 COc1cccc(C(=O)CCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
44400594 140353 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL371165 140353 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
11948707 172946 0 None -53 13 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1021/acs.jmedchem.2c00633
CHEMBL426317 172946 0 None -53 13 Human 7.7 pKi = 7.7 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1021/acs.jmedchem.2c00633
10616050 193425 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48807 193425 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
57326583 80838 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 404 2 0 5 4.7 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022271 80838 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 404 2 0 5 4.7 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
127051845 147507 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3817898 147507 0 None -12 9 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 309 6 0 3 3.7 COc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44426512 92520 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(c1ccc2ccccc2c1)N1CCC(NCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL229076 92520 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(c1ccc2ccccc2c1)N1CCC(NCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
14665503 98009 0 None -346 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 382 7 1 4 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL240106 98009 0 None -346 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 382 7 1 4 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
9977478 211722 2 None -3235 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 386 6 2 5 2.4 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL76402 211722 2 None -3235 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 386 6 2 5 2.4 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
137632607 163118 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 305 3 2 5 1.6 CCCN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4065797 163118 0 None -56 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 305 3 2 5 1.6 CCCN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
1577 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
2537 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
5355 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
5501 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
643497 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
688272 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
958 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
960 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
CHEMBL196677 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
CHEMBL26 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
CHEMBL267044 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
DB00391 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
DB16021 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1021/jm049612a
51354851 66948 0 None -501 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 517 17 1 7 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCOCCOCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1688994 66948 0 None -501 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 517 17 1 7 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCOCCOCCF)cc2)CC1 10.1021/jm101323b
CHEMBL1739761 66948 0 None -501 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 517 17 1 7 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(OCCOCCOCCF)cc2)CC1 10.1021/jm101323b
44578445 188358 0 None -13 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476933 188358 0 None -13 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
1577 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
2537 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
5355 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
5501 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
643497 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
688272 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
958 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
960 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL196677 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL26 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL267044 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
DB00391 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
DB16021 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
137633454 163370 0 None -645 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 645 16 3 10 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
CHEMBL4068702 163370 0 None -645 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 645 16 3 10 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
1577 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
2537 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
5355 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
5501 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
643497 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
688272 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
958 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
960 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL196677 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL26 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL267044 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
DB00391 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
DB16021 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
168289523 198278 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5193761 198278 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.ejmech.2022.114840
168289523 198278 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5193761 198278 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
10692886 60428 3 None -776 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL160296 60428 3 None -776 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813590 60428 3 None -776 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
4797946 177203 7 None 165 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4448320 177203 7 None 165 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 310 4 1 4 2.2 Cc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168275717 196998 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5174731 196998 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.ejmech.2022.114840
2247 7293 81 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 7293 81 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 7293 81 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 7293 81 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 7293 81 None -63 42 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
763774 98924 4 None 16 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420776 98924 4 None 16 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
42626313 63021 0 None -338 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
CHEMBL1627317 63021 0 None -338 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 2 6 2.7 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
10161526 20075 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 9 0 5 6.1 c1ccc(C(c2ccccc2)N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1191882 20075 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 9 0 5 6.1 c1ccc(C(c2ccccc2)N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL543040 20075 0 None -40 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 9 0 5 6.1 c1ccc(C(c2ccccc2)N2CCN(CCCCc3cc(-c4cccs4)no3)CC2)cc1 10.1016/s0960-894x(02)00179-8
44438232 155560 3 None -4 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 2 3 3.7 OC1(c2ccc(Cl)cc2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL394066 155560 3 None -4 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 2 3 3.7 OC1(c2ccc(Cl)cc2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
154705296 183173 1 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4444691 183173 1 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595970 183173 1 None -5 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
168275717 196998 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5174731 196998 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.ejmech.2022.114840
168275717 196998 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5174731 196998 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3ncc4ccccn34)CC2)cc1F 10.1016/j.bmcl.2022.128615
11133385 108963 0 None -6 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.1 O=C(NCCCN1CCN(c2ccccc2)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
CHEMBL302796 108963 0 None -6 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.1 O=C(NCCCN1CCN(c2ccccc2)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
154706703 183011 1 None -38 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4550187 183011 1 None -38 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4594691 183011 1 None -38 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
154706461 183127 1 None -93 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4470439 183127 1 None -93 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595600 183127 1 None -93 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
10613605 207727 0 None -5495 5 Human 5.7 pKi = 5.7 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 292 4 2 2 3.7 c1ccc(CNC[C@H]2CCc3ccc4[nH]ccc4c3O2)cc1 10.1016/s0960-894x(01)00778-8
CHEMBL60185 207727 0 None -5495 5 Human 5.7 pKi = 5.7 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 292 4 2 2 3.7 c1ccc(CNC[C@H]2CCc3ccc4[nH]ccc4c3O2)cc1 10.1016/s0960-894x(01)00778-8
10617381 196465 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL51536 196465 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 343 4 1 3 3.2 Cc1ccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)cc1 10.1016/j.bmcl.2005.02.012
11649431 172761 0 None -91 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 528 11 1 6 4.9 CCCc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL425285 172761 0 None -91 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 528 11 1 6 4.9 CCCc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
10688035 111546 1 None 38 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccccn4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL310819 111546 1 None 38 3 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccccn4)[nH]n3)CC2)cc1 10.1021/jm970111h
4420454 63033 6 None 1 5 Human 7.7 pKi = 7.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 63033 6 None 1 5 Human 7.7 pKi = 7.7 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
10616050 193425 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL48807 193425 3 None 81 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
10131111 215105 0 None 18 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 1 0 3 3.7 CCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL99208 215105 0 None 18 2 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 246 1 0 3 3.7 CCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
10041417 33190 4 None -28 3 Human 7.7 pKi = 7.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1cccs1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL135954 33190 4 None -28 3 Human 7.7 pKi = 7.7 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1cccs1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
10740968 103498 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.1 COc1ccccc1N1CCN(CCNC(=O)C2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL26426 103498 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.1 COc1ccccc1N1CCN(CCNC(=O)C2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
44405451 142126 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2cccc(C(F)(F)F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL372770 142126 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 430 5 1 3 5.4 O=C(N[C@H]1CCN(Cc2cccc(C(F)(F)F)c2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
9908125 126122 0 None 20 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1021/jm0009989
CHEMBL344270 126122 0 None 20 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1021/jm0009989
44436597 98575 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241210 98575 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
71734127 97832 0 None -4 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
CHEMBL2397476 97832 0 None -4 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
46917637 75107 0 None -18 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916548 75107 0 None -18 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
10861560 52107 10 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1ccc(N2CCN(CCNC(=O)c3cccc(OC)c3)CC2)cc1 10.1021/jm020952a
CHEMBL152679 52107 10 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 369 7 1 5 2.3 COc1ccc(N2CCN(CCNC(=O)c3cccc(OC)c3)CC2)cc1 10.1021/jm020952a
11280344 98932 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 376 3 0 3 5.5 Clc1cccc(N2CCN(Cc3csc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420891 98932 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 376 3 0 3 5.5 Clc1cccc(N2CCN(Cc3csc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
44283941 144708 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 336 4 1 4 2.4 Cc1ccnc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)c1 10.1016/s0960-894x(98)00252-2
CHEMBL37638 144708 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 336 4 1 4 2.4 Cc1ccnc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)c1 10.1016/s0960-894x(98)00252-2
11324794 145037 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL377050 145037 0 None 7 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 324 6 0 5 2.6 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
90644063 118812 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
CHEMBL3289648 118812 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
90644063 118812 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 118812 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
76328715 113149 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115582 113149 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139265 113149 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
133633 9021 53 None -104 8 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm9600712
177 9021 53 None -104 8 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm9600712
CHEMBL445102 9021 53 None -104 8 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm9600712
44380774 127253 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL354180 127253 0 None -13 4 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
154704141 183458 1 None -9 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4561808 183458 1 None -9 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4598299 183458 1 None -9 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
49783042 24463 0 None -7 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 1 3 4.3 Cc1ccc(C)c(C(=O)NCCCCN2CCN(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1258495 24463 0 None -7 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 393 7 1 3 4.3 Cc1ccc(C)c(C(=O)NCCCCN2CCN(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
57390115 76071 0 None -44 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928120 76071 0 None -44 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
44436601 98718 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(C#Cc3ccccc3)cc2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL241424 98718 0 None -21 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(C#Cc3ccccc3)cc2)CC1 10.1016/j.bmc.2007.08.038
10830804 214701 0 None 6 2 Human 5.7 pKi = 5.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 337 5 3 4 1.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCNC1 10.1021/jm9601720
CHEMBL96792 214701 0 None 6 2 Human 5.7 pKi = 5.7 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 337 5 3 4 1.8 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCNC1 10.1021/jm9601720
2337 10030 77 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
50 10030 77 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
5002 10030 77 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL716 10030 77 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
DB01224 10030 77 None -114 62 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
10438027 72962 0 None -645 6 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1016/j.bmcl.2004.05.052
CHEMBL184383 72962 0 None -645 6 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1016/j.bmcl.2004.05.052
142590710 187049 0 None -3 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(Cc1ccccc1)CN1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4750607 187049 0 None -3 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(Cc1ccccc1)CN1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
118709166 120189 0 None -39 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 25 0 8 12.9 O=C(CCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318838 120189 0 None -39 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 25 0 8 12.9 O=C(CCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
12071089 12077 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 8 0 2 7.1 Clc1cccc(C(OC2CC3CCC(C2)N3CCCc2ccccc2)c2ccccc2)c1 10.1021/jm010146o
CHEMBL106660 12077 0 None -3 3 Human 6.7 pKi = 6.7 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 445 8 0 2 7.1 Clc1cccc(C(OC2CC3CCC(C2)N3CCCc2ccccc2)c2ccccc2)c1 10.1021/jm010146o
122180610 128516 0 None -40 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 4.0 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588981 128516 0 None -40 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 4.0 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
44426513 92521 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(c1ccc2ccccc2c1)N1CCC(NCCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL229077 92521 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(c1ccc2ccccc2c1)N1CCC(NCCCc2ccccc2)CC1 10.1016/j.bmcl.2006.12.096
154706546 183225 1 None -48 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4452329 183225 1 None -48 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4596339 183225 1 None -48 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
44431472 94257 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL233403 94257 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
49799713 21181 0 None -177 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1ccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1173778 21181 0 None -177 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1ccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1200306 21181 0 None -177 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 376 4 2 4 3.7 COc1ccc2[nH]cc(CN3CCC(n4c(=O)[nH]c5ccccc54)CC3)c2c1 10.1016/j.bmc.2010.05.052
162666450 189068 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4783987 189068 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
10225942 19926 0 None -147 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 9 0 4 6.1 c1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1190732 19926 0 None -147 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 9 0 4 6.1 c1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL541524 19926 0 None -147 3 Human 5.7 pKi = 5.7 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 9 0 4 6.1 c1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
45379370 14295 0 None -21 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
CHEMBL1087301 14295 0 None -21 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
16744003 99333 0 None -43 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
CHEMBL243225 99333 0 None -43 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
162666450 189068 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4783987 189068 0 None -15 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3ccc(-c4ccccc4)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
17755866 149662 1 None -162 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
CHEMBL389356 149662 1 None -162 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
9929581 23286 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 376 3 0 4 4.4 CC(C)(C)c1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL123663 23286 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 376 3 0 4 4.4 CC(C)(C)c1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
118719810 122516 0 None -100 4 Human 6.6 pKi = 6.6 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 451 10 0 7 4.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353914 122516 0 None -100 4 Human 6.6 pKi = 6.6 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 451 10 0 7 4.5 COc1ccccc1N1CCN(CCCCCc2cn(-c3ccc(SC)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
44438222 100266 0 None -11 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 349 3 1 2 4.9 N#CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246230 100266 0 None -11 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 349 3 1 2 4.9 N#CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10425024 13908 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1021/jm950721m
CHEMBL108531 13908 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1021/jm950721m
9794644 114058 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317078 114058 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 232 0 0 3 3.3 Cc1sc(C)c2c1CCCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
127051863 147592 0 None 1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 384 6 1 4 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818940 147592 0 None 1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 384 6 1 4 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
10425024 13908 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL108531 13908 4 None -40 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 302 3 1 2 3.8 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL5283077 200964 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 0 5 2.9 c1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)nc1 10.1016/j.ejmech.2022.114840
CHEMBL5283077 200964 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 0 5 2.9 c1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)nc1 10.1016/j.ejmech.2022.114840
44438219 174452 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 339 3 2 2 4.3 NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL430198 174452 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 339 3 2 2 4.3 NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10688036 110922 0 None 38 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4cccnc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL309460 110922 0 None 38 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4cccnc4)[nH]n3)CC2)cc1 10.1021/jm970111h
10735344 111635 0 None 52 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.4 c1ccc(CCN2CCN(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL310985 111635 0 None 52 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.4 c1ccc(CCN2CCN(c3cc(-c4ccccc4)[nH]n3)CC2)cc1 10.1021/jm970111h
10381810 211953 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL7828 211953 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ccccc32)CC1 10.1021/jm00043a008
44381118 64343 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL166587 64343 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
44356064 123324 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL336295 123324 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 329 7 0 3 4.6 CCCN(CCc1cccs1)[C@@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
90644063 118812 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
CHEMBL3289648 118812 0 None 1 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2020.115943
90644063 118812 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 118812 0 None -1 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
49783040 24462 0 None -4 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 395 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc(C)ccc2C)CC1 10.1021/jm100899z
CHEMBL1258494 24462 0 None -4 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 395 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc(C)ccc2C)CC1 10.1021/jm100899z
72544789 99907 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443010 99907 0 None 9 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
11417962 11746 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 392 7 0 6 3.5 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104873 11746 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 392 7 0 6 3.5 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
10832341 214632 0 None 218 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 359 7 1 4 3.3 COc1cccc(CNCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL96462 214632 0 None 218 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 359 7 1 4 3.3 COc1cccc(CNCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
168278360 199626 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 377 7 0 3 4.0 O=C1CCc2ccccc2N1CCCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5188796 199626 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 377 7 0 3 4.0 O=C1CCc2ccccc2N1CCCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221749 199626 0 None 8 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 377 7 0 3 4.0 O=C1CCc2ccccc2N1CCCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
11089541 91161 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 354 6 1 5 2.0 COc1cccc(C(=O)NCCN2CCN(c3cc(C)ccn3)CC2)c1 10.1021/jm020952a
CHEMBL2112905 91161 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 354 6 1 5 2.0 COc1cccc(C(=O)NCCN2CCN(c3cc(C)ccn3)CC2)c1 10.1021/jm020952a
CHEMBL2219567 91161 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 354 6 1 5 2.0 COc1cccc(C(=O)NCCN2CCN(c3cc(C)ccn3)CC2)c1 10.1021/jm020952a
9883554 172133 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL423659 172133 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
10071413 90745 0 None -41 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3[nH]2)CC1 10.1021/jm0611152
CHEMBL220700 90745 0 None -41 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3[nH]2)CC1 10.1021/jm0611152
35295787 92516 3 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL229021 92516 3 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 5 1 2 4.3 O=C(NC1CCN(CCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
44336571 11603 0 None 30 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
CHEMBL104201 11603 0 None 30 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
52937680 67947 0 None -416 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 466 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1Cc2cccn3ncc(c23)C1 10.1021/jm101639t
CHEMBL1765632 67947 0 None -416 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 466 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1Cc2cccn3ncc(c23)C1 10.1021/jm101639t
9838216 209967 1 None -12 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 266 6 2 2 3.3 c1ccc(CNCCOc2cccc3[nH]ccc23)cc1 10.1016/s0960-894x(99)00434-5
CHEMBL64283 209967 1 None -12 5 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 266 6 2 2 3.3 c1ccc(CNCCOc2cccc3[nH]ccc23)cc1 10.1016/s0960-894x(99)00434-5
130431279 182663 0 None -102 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 254 3 1 3 2.3 CCc1cc(Cl)c(OC)c(N2CCNCC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4586327 182663 0 None -102 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 254 3 1 3 2.3 CCc1cc(Cl)c(OC)c(N2CCNCC2)c1 10.1021/acs.jmedchem.6b00860
44264741 211521 0 None 1 3 Human 4.6 pKi = 4.6 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 340 2 0 4 3.0 O=C(c1cnn2ccccc12)N1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7441 211521 0 None 1 3 Human 4.6 pKi = 4.6 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 340 2 0 4 3.0 O=C(c1cnn2ccccc12)N1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00692-1
10300403 20502 0 None -120 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 496 10 0 6 6.0 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1195074 20502 0 None -120 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 496 10 0 6 6.0 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
CHEMBL553810 20502 0 None -120 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 496 10 0 6 6.0 O=[N+]([O-])c1cccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)c1 10.1016/s0960-894x(02)00179-8
122180575 128505 0 None -21 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.7 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588920 128505 0 None -21 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.7 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
24060 126433 12 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 264 5 0 2 3.4 CN(C)CCC(C#N)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL346898 126433 12 None -6 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 264 5 0 2 3.4 CN(C)CCC(C#N)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
154725813 183305 1 None -89 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4568916 183305 1 None -89 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4597047 183305 1 None -89 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
44276079 20572 0 None -11 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 439 9 0 6 4.6 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4F)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1195587 20572 0 None -11 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 439 9 0 6 4.6 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4F)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL554897 20572 0 None -11 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 439 9 0 6 4.6 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4F)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
56664952 73158 0 None -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 9 1 5 4.0 COc1ccccc1N1CCN(CCCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813598 73158 0 None -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 9 1 5 4.0 COc1ccccc1N1CCN(CCCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851753 73158 0 None -33 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 9 1 5 4.0 COc1ccccc1N1CCN(CCCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
9928332 103955 5 None -117 9 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D4Inhibition of [3H]spiperone binding to Dopamine receptor D4
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1021/jm049619s
CHEMBL268258 103955 5 None -117 9 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D4Inhibition of [3H]spiperone binding to Dopamine receptor D4
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1021/jm049619s
CHEMBL5083186 221629 0 None -1202 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
44336172 12133 0 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 476 6 0 5 2.3 CN(C)S(=O)(=O)c1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106917 12133 0 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 476 6 0 5 2.3 CN(C)S(=O)(=O)c1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44336194 114316 1 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 5 0 4 3.8 CSc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL318760 114316 1 None 16 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 5 0 4 3.8 CSc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
122181334 128654 0 None -954 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 442 7 2 5 3.4 Cc1ccc(Cl)c(N2CCN(CCCCNC(=O)c3ccc4oc(=O)[nH]c4c3)CC2)c1 10.1021/jm501512b
CHEMBL3590086 128654 0 None -954 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 442 7 2 5 3.4 Cc1ccc(Cl)c(N2CCN(CCCCNC(=O)c3ccc4oc(=O)[nH]c4c3)CC2)c1 10.1021/jm501512b
130431317 179729 0 None -2454 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4517102 179729 0 None -2454 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
164628177 195390 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4875079 195390 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL5029038 195390 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
168281091 197850 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5187429 197850 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.ejmech.2022.114840
10404657 104845 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL273241 104845 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
11213037 143881 0 None -851 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 3 5.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm0611152
CHEMBL374749 143881 0 None -851 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 3 5.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm0611152
71618702 150160 0 None -5 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@H](COc2cccc(Cl)c2)C1 nan
CHEMBL3897835 150160 0 None -5 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 400 5 0 4 3.4 CC1Cc2ccccc2N1C(=O)CN1CCO[C@H](COc2cccc(Cl)c2)C1 nan
90644070 118818 0 None -3 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 366 5 0 3 5.0 Clc1ccc(N2C[C@H]3C[C@@H]2CN3CCCc2cc3ccccc3o2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289654 118818 0 None -3 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 366 5 0 3 5.0 Clc1ccc(N2C[C@H]3C[C@@H]2CN3CCCc2cc3ccccc3o2)cc1 10.1016/j.bmc.2014.04.026
164628177 195390 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4875079 195390 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL5029038 195390 0 None -25 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 7 1 5 2.8 CC(=O)Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
44394636 73692 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL186558 73692 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
44214765 172579 0 None 208 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 371 5 2 3 3.9 Nc1cccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL424808 172579 0 None 208 2 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 371 5 2 3 3.9 Nc1cccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)c1 10.1016/j.bmcl.2004.07.045
219050 10146 25 None -58 21 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
52 10146 25 None -58 21 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
CHEMBL431367 10146 25 None -58 21 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10.1021/jm950721m
13015797 212676 0 None 1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 400 6 0 5 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3ccc(F)cc3)CC1)OCC2 10.1021/jm960084f
CHEMBL83915 212676 0 None 1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 400 6 0 5 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3ccc(F)cc3)CC1)OCC2 10.1021/jm960084f
9888555 172383 16 None -208 8 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm100899z
CHEMBL424294 172383 16 None -208 8 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm100899z
136056636 118565 0 None -28 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287404 118565 0 None -28 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
118709159 120182 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 832 17 0 8 9.7 O=C(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318831 120182 0 None -3 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 832 17 0 8 9.7 O=C(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
11156017 11898 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 487 7 0 4 4.6 CCOc1cc(I)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105686 11898 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 487 7 0 4 4.6 CCOc1cc(I)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
9927411 209832 0 None 4 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
CHEMBL63576 209832 0 None 4 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
9797200 125749 0 None 109 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 321 4 1 3 2.7 O=C1NC(CCN2CCN(c3ccccc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
CHEMBL34239 125749 0 None 109 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 321 4 1 3 2.7 O=C1NC(CCN2CCN(c3ccccc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
45482153 204817 0 None -5 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 502 9 1 7 3.9 COc1ccc(-n2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
CHEMBL574030 204817 0 None -5 4 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 502 9 1 7 3.9 COc1ccc(-n2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
44380785 127581 0 None -7 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL355566 127581 0 None -7 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
10404657 104845 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
CHEMBL273241 104845 0 None -28 5 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 334 5 0 3 3.1 O=C1c2ccccc2C(=O)N1CCCCN1CCc2ccccc2C1 10.1016/j.bmc.2016.05.053
90644064 118813 0 None -1 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 383 7 0 4 5.0 Clc1ccc(N2CCN(CCCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289649 118813 0 None -1 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 383 7 0 4 5.0 Clc1ccc(N2CCN(CCCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
57390117 76074 0 None -16 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928123 76074 0 None -16 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
127047221 146708 0 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3799593 146708 0 None 1 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
57400562 76093 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928247 76093 0 None -2 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
71086389 167187 0 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4111289 167187 0 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
10811814 214244 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL94265 214244 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
154704941 183406 1 None -7 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4578364 183406 1 None -7 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597877 183406 1 None -7 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
168281091 197850 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5187429 197850 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.ejmech.2022.114840
10811814 214244 0 None - 1 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL94265 214244 0 None - 1 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 415 9 1 4 4.1 COc1cccc(C(=O)NCCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
168281091 197850 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5187429 197850 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccc(C)cc3)C2)cc1F 10.1016/j.bmcl.2022.128615
182600 125522 2 None -2 3 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 352 5 0 3 3.9 O=C(CCCN1CCN2c3ccccc3CCC2C1)c1ccc(F)cc1 10.1021/jm049031l
CHEMBL341774 125522 2 None -2 3 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 352 5 0 3 3.9 O=C(CCCN1CCN2c3ccccc3CCC2C1)c1ccc(F)cc1 10.1021/jm049031l
10229397 20028 0 None -123 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1191467 20028 0 None -123 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL542571 20028 0 None -123 3 Human 5.6 pKi = 5.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 511 11 0 6 6.1 COc1ccc(-c2cc(CCCCN3CCN(C(c4ccccc4)c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
44438215 100185 5 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmcl.2006.10.076
CHEMBL245816 100185 5 None 1 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmcl.2006.10.076
9906978 49485 2 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 49485 2 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
49798812 21092 0 None -16 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1170456 21092 0 None -16 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1199971 21092 0 None -16 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
9906978 49485 2 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL150161 49485 2 None 1 12 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
23290944 88601 0 None -323 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164350 88601 0 None -323 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
51353989 66983 0 None -112 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 481 11 1 5 5.1 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1689006 66983 0 None -112 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 481 11 1 5 5.1 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
CHEMBL1739963 66983 0 None -112 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 481 11 1 5 5.1 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(-c2ccsc2)cc1 10.1021/jm101323b
9908071 209783 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 3 0 3 3.4 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL63209 209783 0 None 3 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 3 0 3 3.4 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
21533446 76930 0 None -6 10 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
CHEMBL1940403 76930 0 None -6 10 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmc.2011.12.019
90181059 167010 0 None -1 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
CHEMBL4109801 167010 0 None -1 4 Mouse 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
44339879 179061 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL447476 179061 0 None 4 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
11792324 212508 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL82591 212508 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CC[C@H]3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
10851078 206169 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
CHEMBL59103 206169 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
10644771 113866 0 None 15 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL315879 113866 0 None 15 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
44335761 115998 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL321734 115998 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 379 5 0 4 2.8 COc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
10851078 206169 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
CHEMBL59103 206169 1 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 290 3 1 1 4.5 c1ccc(C2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
145988693 173945 0 None 5 17 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 173945 0 None 5 17 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
45268293 202914 0 None 20 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 408 4 1 7 1.4 Cn1c(N2CCOCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL561123 202914 0 None 20 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 408 4 1 7 1.4 Cn1c(N2CCOCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
10644771 113866 0 None 15 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL315879 113866 0 None 15 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 401 8 1 4 3.7 COc1cccc(C(=O)NCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
44301157 108483 0 None 79 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 343 5 0 3 4.4 O=C(OCC1CCN(Cc2ccccc2)CC1)c1ccc(Cl)cc1 10.1021/jm960017l
CHEMBL299479 108483 0 None 79 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 343 5 0 3 4.4 O=C(OCC1CCN(Cc2ccccc2)CC1)c1ccc(Cl)cc1 10.1021/jm960017l
10595646 206136 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.5 COc1cc2ccccc2cc1OCCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL59075 206136 0 None 63 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.5 COc1cc2ccccc2cc1OCCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
42266974 106071 9 None 100 2 Human 7.6 pKi = 7.6 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 323 4 1 3 2.6 CC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL282008 106071 9 None 100 2 Human 7.6 pKi = 7.6 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 323 4 1 3 2.6 CC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
2726 7706 68 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
621 7706 68 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
83 7706 68 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
CHEMBL71 7706 68 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
DB00477 7706 68 None -8 72 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm070516u
11185987 87123 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL214314 87123 0 None 10 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 310 5 1 5 2.5 O/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
16094666 88502 3 None 52 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL216393 88502 3 None 52 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 308 4 1 2 3.8 Cc1cccc(NC(=O)CN2CCC(c3ccccc3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL5089655 221999 0 None 2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10089203 48127 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 349 4 1 6 3.1 CNc1nc(Cl)c(Sc2ccccc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL14899 48127 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 349 4 1 6 3.1 CNc1nc(Cl)c(Sc2ccccc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
233199 162390 16 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 286 3 0 2 3.7 Clc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
CHEMBL404570 162390 16 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 286 3 0 2 3.7 Clc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
44380717 127127 0 None 10 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL353087 127127 0 None 10 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
23642427 98574 0 None -549 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 430 7 1 4 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL241169 98574 0 None -549 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 430 7 1 4 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
57395340 76075 0 None -28 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928124 76075 0 None -28 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
11774358 11925 0 None - 1 Human 6.6 pKi = 6.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 415 6 0 4 4.6 COc1ccc(C(F)(F)F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105836 11925 0 None - 1 Human 6.6 pKi = 6.6 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 415 6 0 4 4.6 COc1ccc(C(F)(F)F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
12049520 107842 5 None 9 4 Human 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 319 4 0 4 3.7 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)co2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL294780 107842 5 None 9 4 Human 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 319 4 0 4 3.7 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)co2)cc1 10.1016/s0960-894x(00)00405-4
10449136 214210 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL94067 214210 0 None 1 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10014924 114048 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
CHEMBL316983 114048 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
10014924 114048 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
CHEMBL316983 114048 0 None -16 5 Human 5.6 pKi = 5.6 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
18519 74434 27 None 1 2 Human 5.6 pKi = 5.6 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 287 2 5 5 1.9 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1O 10.1016/S0960-894X(97)00194-7
CHEMBL19068 74434 27 None 1 2 Human 5.6 pKi = 5.6 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 287 2 5 5 1.9 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1O 10.1016/S0960-894X(97)00194-7
134155116 157747 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3958215 157747 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
242 7258 124 None -104 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
34 7258 124 None -104 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
60795 7258 124 None -104 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL1112 7258 124 None -104 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
DB01238 7258 124 None -104 51 Human 6.6 pKi = 6.6 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
155547197 180374 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4533305 180374 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
134155116 157747 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3958215 157747 0 None -158 7 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 309 3 0 2 3.6 O=C1c2ccc(F)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
11540842 91148 0 None -29 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 514 10 1 6 4.7 Cc1c(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL221897 91148 0 None -29 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 514 10 1 6 4.7 Cc1c(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
9872676 84970 0 None -6309 17 Human 5.6 pKi = 5.6 Binding
Binding affinity to human D4.4 receptorBinding affinity to human D4.4 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 84970 0 None -6309 17 Human 5.6 pKi = 5.6 Binding
Binding affinity to human D4.4 receptorBinding affinity to human D4.4 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
11522476 81298 0 None -4 3 Human 5.6 pKi = 5.6 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
CHEMBL202924 81298 0 None -4 3 Human 5.6 pKi = 5.6 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
71453386 88596 0 None -17 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1cccc2ccccc12)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164345 88596 0 None -17 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1cccc2ccccc12)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
4987774 21131 1 None -14 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172210 21131 1 None -14 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200151 21131 1 None -14 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2cc3ccccc3o2)CC1 10.1016/j.bmc.2010.05.052
10801925 18396 1 None -9 5 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL1180675 18396 1 None -9 5 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@H](CNCc1ccccc1)CC2 10.1021/jm9703653
CHEMBL138016 18396 1 None -9 5 Human 6.6 pKi = 6.6 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@H](CNCc1ccccc1)CC2 10.1021/jm9703653
44330340 114252 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 275 2 1 3 3.3 Cc1sc(C)c2c1CCCc1c(CN(C)C)n[nH]c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL318415 114252 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 275 2 1 3 3.3 Cc1sc(C)c2c1CCCc1c(CN(C)C)n[nH]c1-2 10.1016/s0960-894x(03)00587-0
46227317 206942 0 None -14 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL596448 206942 0 None -14 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
155547197 180374 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4533305 180374 0 None -208 7 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 341 6 0 4 3.4 O=C(CCCN1CCCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
11633816 19897 3 None -48 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1190494 19897 3 None -48 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL541025 19897 3 None -48 3 Human 6.6 pKi = 6.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
137640511 163845 0 None 14 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4074104 163845 0 None 14 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 286 4 0 2 3.1 CC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
23363843 116448 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 4 2.7 O=C1C(=O)N(CCN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL322567 116448 0 None 4 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 4 2.7 O=C1C(=O)N(CCN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
44370058 126472 0 None 19 3 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 336 5 1 4 2.9 COc1ccc(N2CCN(CCc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
CHEMBL347291 126472 0 None 19 3 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 336 5 1 4 2.9 COc1ccc(N2CCN(CCc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(99)00025-6
10357628 20695 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 303 2 0 2 5.0 CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1196433 20695 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 303 2 0 2 5.0 CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL556969 20695 0 None -1 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 303 2 0 2 5.0 CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
10474613 170070 0 None 54 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 375 7 1 3 4.5 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL418758 170070 0 None 54 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 375 7 1 3 4.5 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10176799 215041 0 None 17 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL98830 215041 0 None 17 2 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
127029389 146221 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793984 146221 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3cccc(F)c3)C2)cc1 10.1016/j.bmcl.2016.03.102
44431488 94850 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.106
CHEMBL234647 94850 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccccc1CN1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.106
22100933 211069 4 None 22 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc2[nH]c(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
CHEMBL71324 211069 4 None 22 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc2[nH]c(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
44371980 60709 0 None 7 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 514 6 0 6 4.9 Cc1nn2c(N3CCN(Cc4ccccc4)CC3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160536 60709 0 None 7 4 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 514 6 0 6 4.9 Cc1nn2c(N3CCN(Cc4ccccc4)CC3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
1353 8692 93 None -3 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
3559 8692 93 None -3 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
86 8692 93 None -3 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL54 8692 93 None -3 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
DB00502 8692 93 None -3 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.1c01327
11220975 109770 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
CHEMBL306711 109770 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
5311346 210933 28 None -19 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/acs.jmedchem.9b00702
CHEMBL1256778 210933 28 None -19 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/acs.jmedchem.9b00702
CHEMBL70565 210933 28 None -19 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/acs.jmedchem.9b00702
10665101 108302 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
CHEMBL298166 108302 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1016/j.bmcl.2005.02.012
9883554 172133 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL423659 172133 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
10498972 125237 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL341225 125237 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
44269825 49286 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 368 3 0 5 4.0 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL14998 49286 0 None -4 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 368 3 0 5 4.0 Cc1nc(Cl)c(Sc2ccc(Cl)cc2)c(N2CCN(C)CC2)n1 10.1016/s0960-894x(01)00167-6
CHEMBL5277859 200734 0 None 38 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to human D4R assessed as inhibition constantBinding affinity to human D4R assessed as inhibition constant
ChEMBL 348 4 0 5 2.8 CCOC(=O)N1CCN(Cc2cnn(-c3ccc(Cl)cc3)c2)CC1 10.1016/j.ejmech.2020.113141
CHEMBL5277859 200734 0 None 38 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-nemonapride from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 348 4 0 5 2.8 CCOC(=O)N1CCN(Cc2cnn(-c3ccc(Cl)cc3)c2)CC1 10.1016/j.ejmech.2020.113141
CHEMBL4434865 220702 1 None 23 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None c1ccc(Cc2cn(C3CCN(Cc4ccccc4)CC3)nn2)cc1 10.1016/j.bmc.2022.116851
25141534 63009 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1016/j.bmc.2015.01.017
CHEMBL1627305 63009 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1016/j.bmc.2015.01.017
25141534 63009 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
CHEMBL1627305 63009 0 None -1698 7 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
137637428 163015 0 None -3 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 250 1 1 5 0.9 CN1CCN(c2ccc(O)c3c2OCCO3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4064759 163015 0 None -3 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 250 1 1 5 0.9 CN1CCN(c2ccc(O)c3c2OCCO3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL5076359 221211 0 None -77 4 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None COc1cccc(C(=CCNCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2cccc(OC)c2)c1 10.1021/acs.jmedchem.1c00611
181743 185351 5 None -131 22 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptorDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 185351 5 None -131 22 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptorDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
1605 9276 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
1728 9276 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
22267 9276 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
4095 9276 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
4586 9276 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
5458 9276 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
CHEMBL159659 9276 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
CHEMBL651 9276 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
DB00333 9276 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
DB13515 9276 24 None -8511 10 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)C[C@H](N(C)C)C 10.1021/acs.jmedchem.1c00611
11488451 209929 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 478 8 1 6 3.3 COc1cc2c(cc1OC)CN(CCNC(=O)c1cc(Br)cc(OC)c1OC)CC2 10.1016/j.bmcl.2003.09.083
CHEMBL64176 209929 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 478 8 1 6 3.3 COc1cc2c(cc1OC)CN(CCNC(=O)c1cc(Br)cc(OC)c1OC)CC2 10.1016/j.bmcl.2003.09.083
10782097 121041 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.4 CCN(CCNCc1ccc2ccc(=O)oc2c1)c1ccccc1 10.1021/jm990266k
CHEMBL333057 121041 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.4 CCN(CCNCc1ccc2ccc(=O)oc2c1)c1ccccc1 10.1021/jm990266k
511484 11116 71 None -6 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 252 3 0 2 3.0 c1ccc(CN2CCN(c3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL101032 11116 71 None -6 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 252 3 0 2 3.0 c1ccc(CN2CCN(c3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
142590755 190205 0 None -3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(CNC1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2020.112674
CHEMBL4798638 190205 0 None -3 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 496 11 2 4 5.4 OC(CNC1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1)Cc1ccccc1 10.1016/j.ejmech.2020.112674
CHEMBL5274285 200585 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 415 4 1 2 5.3 Fc1ccc(CN2CCCC23CCN(Cc2cc4ccc(Cl)cc4[nH]2)C3)cc1F 10.1016/j.ejmech.2022.114840
10058787 123372 0 None -407 3 Human 6.6 pKi = 6.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL336652 123372 0 None -407 3 Human 6.6 pKi = 6.6 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2ccc(O)cc2C1 10.1021/jm960345l
122180611 128517 0 None -39 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 442 8 0 7 4.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ncccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588982 128517 0 None -39 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 442 8 0 7 4.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4ncccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
134154680 161341 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3959919 161341 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3991166 161341 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL5274285 200585 0 None -2 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 415 4 1 2 5.3 Fc1ccc(CN2CCCC23CCN(Cc2cc4ccc(Cl)cc4[nH]2)C3)cc1F 10.1016/j.ejmech.2022.114840
11613105 90843 0 None -39 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 506 12 1 8 3.4 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
CHEMBL220754 90843 0 None -39 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 506 12 1 8 3.4 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
44339992 115961 0 None 22 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL321492 115961 0 None 22 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10665101 108302 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
CHEMBL298166 108302 0 None 22 3 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 343 4 1 3 3.2 Cc1cccc(C(=O)NCN2CCN(c3ccccc3Cl)CC2)c1 10.1021/jm970021c
9883554 172133 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
CHEMBL423659 172133 0 None 141 2 Human 7.6 pKi = 7.6 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 320 4 1 4 2.1 N#Cc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1021/jm970021c
10498972 125237 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
CHEMBL341225 125237 1 None 63 3 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 363 9 1 3 4.2 Cc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
44336313 16016 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL110712 16016 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00656-x
9883552 22358 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2ccc(CN3CCN(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL122140 22358 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2ccc(CN3CCN(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
127031497 146269 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3794469 146269 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 351 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
145969667 171744 0 None -1 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 171744 0 None -1 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
118709751 120318 0 None -20 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
CHEMBL3321792 120318 0 None -20 10 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
21219144 100115 0 None 40 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL24539 100115 0 None 40 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 319 4 0 5 3.2 c1ccc(CN2CCC(n3nnc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(99)00169-9
10939167 16272 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL112065 16272 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL129483 16272 0 None -7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
44332566 115136 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 276 6 2 3 3.1 Nc1cc(OCCNCc2ccccc2)ccc1Cl 10.1016/s0960-894x(98)00014-6
CHEMBL319816 115136 0 None 8 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 276 6 2 3 3.1 Nc1cc(OCCNCc2ccccc2)ccc1Cl 10.1016/s0960-894x(98)00014-6
56681927 73170 1 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 8 1 5 3.9 COc1cc(C)ccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813593 73170 1 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 8 1 5 3.9 COc1cc(C)ccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851787 73170 1 None -5 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 423 8 1 5 3.9 COc1cc(C)ccc1N1CCN(CCCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
11221906 86686 0 None 5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
CHEMBL212444 86686 0 None 5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 352 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(C)c(C)c1 10.1021/jm060279f
76328715 113149 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115582 113149 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139265 113149 0 None -2 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 429 9 2 6 2.8 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
9841608 107199 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 355 4 1 3 3.3 O=C1NC(CCN2CCN(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
CHEMBL290351 107199 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 355 4 1 3 3.3 O=C1NC(CCN2CCN(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(98)00252-2
10449136 214210 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL94067 214210 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
10449136 214210 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL94067 214210 0 None 1 3 Human 6.6 pKi = 6.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 327 1 0 1 5.6 CC(C)=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
137640836 163785 0 None -31 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 434 7 1 8 3.1 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2o1 10.1021/acs.jmedchem.7b00363
CHEMBL4073330 163785 0 None -31 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 434 7 1 8 3.1 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2o1 10.1021/acs.jmedchem.7b00363
17987129 118196 2 None - 1 Human 5.6 pKi = 5.6 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 323 5 2 2 3.2 O=C(NCc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL327339 118196 2 None - 1 Human 5.6 pKi = 5.6 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 323 5 2 2 3.2 O=C(NCc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
13014681 211508 0 None -891 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.1 CN1CCC(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL7430 211508 0 None -891 3 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 323 1 0 1 5.1 CN1CCC(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
44323876 213361 0 None -22 4 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL88870 213361 0 None -22 4 Human 5.6 pKi = 5.6 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
10568740 22328 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 4 0 4 3.1 O=c1ccc2ccc(CN3CCN(Cc4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL121967 22328 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 4 0 4 3.1 O=c1ccc2ccc(CN3CCN(Cc4ccccc4)CC3)cc2o1 10.1021/jm990266k
15508239 13028 0 None 2 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 336 3 0 2 4.6 C[Si](C)(C)C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL108160 13028 0 None 2 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 336 3 0 2 4.6 C[Si](C)(C)C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
44582678 188353 0 None -18 10 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 188353 0 None -18 10 Human 5.6 pKi = 5.6 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
17756101 105360 1 None -79 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL276778 105360 1 None -79 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
134154680 161341 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3959919 161341 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
CHEMBL3991166 161341 0 None -38 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 416 7 0 5 5.3 COc1cc2c(cc1OC)CN(CCCCc1nc3cc(Cl)ccc3s1)CC2 10.1016/j.bmc.2016.09.019
9904074 117405 3 None -190 3 Human 6.6 pKi = 6.6 Binding
in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2cc3nc(N)sc3cc2C1 10.1021/jm000087z
CHEMBL325710 117405 3 None -190 3 Human 6.6 pKi = 6.6 Binding
in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
ChEMBL 289 5 1 4 3.5 CCCN(CCC)C1Cc2cc3nc(N)sc3cc2C1 10.1021/jm000087z
44330692 119145 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 202 0 1 2 2.8 Cc1oc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL329503 119145 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 202 0 1 2 2.8 Cc1oc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
10357631 14761 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1016/j.bmcl.2005.02.012
CHEMBL109063 14761 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1016/j.bmcl.2005.02.012
168296363 199296 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5209344 199296 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
155557792 181464 0 None -69 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1OCCOC1(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.02.056
CHEMBL4559278 181464 0 None -69 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1OCCOC1(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2019.02.056
44438218 100224 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246020 100224 0 None -2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 338 3 1 1 5.4 CC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
168296363 199296 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5209344 199296 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
168296363 199296 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5209344 199296 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.0 Cn1ncc2cc(CN3CCC(OCc4ccc(F)c(F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
17756212 93143 1 None -36 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL231374 93143 1 None -36 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
7077 73733 27 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL186720 73733 27 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL3925724 73733 27 None -10 5 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
15034333 11022 1 None -2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccc(OCCNCc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL100461 11022 1 None -2 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccc(OCCNCc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
44591042 183590 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
CHEMBL460854 183590 0 None -15 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
10357631 14761 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1021/jm950721m
CHEMBL109063 14761 0 None -38 4 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)cn1 10.1021/jm950721m
CHEMBL5087543 221886 0 None -46 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
134153539 161284 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3971383 161284 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990611 161284 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
10017758 19956 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 2 0 1 4.8 CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1190993 19956 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 2 0 1 4.8 CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL542029 19956 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 2 0 1 4.8 CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
45482169 204617 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 559 12 1 8 4.5 O=C(CCCc1cn(-c2ccc([N+](=O)[O-])cc2)nn1)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2009.06.041
CHEMBL572379 204617 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 559 12 1 8 4.5 O=C(CCCc1cn(-c2ccc([N+](=O)[O-])cc2)nn1)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2009.06.041
135398745 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
47 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
CHEMBL715 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
DB00334 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
135398745 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
47 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
CHEMBL715 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
DB00334 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
155548336 180519 0 None 14 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 8 2 4 4.5 O=C(NCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4536530 180519 0 None 14 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 507 8 2 4 4.5 O=C(NCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
127029391 146126 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792907 146126 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1cc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)ccc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL5282085 200921 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 5 3.1 Cn1ncc2cc(CN3CCO[C@H](COc4ccc(F)c(F)c4)C3)ccc21 10.1016/j.ejmech.2022.114840
118709750 120317 0 None -2 9 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
CHEMBL3321791 120317 0 None -2 9 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1cccc(F)c1 10.1016/j.bmcl.2014.07.018
16105548 89473 0 None -75 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
CHEMBL217964 89473 0 None -75 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
CHEMBL221652 89473 0 None -75 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
10073194 19735 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 465 11 0 7 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccc(OC)c(OC)c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1189407 19735 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 465 11 0 7 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccc(OC)c(OC)c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL538723 19735 0 None -10 3 Human 7.6 pKi = 7.6 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 465 11 0 7 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccc(OC)c(OC)c3)no2)CC1 10.1016/s0960-894x(02)00179-8
135398745 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
47 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
CHEMBL715 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
DB00334 9688 112 None -10 65 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm401958n
118714552 121305 0 None 97 2 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335555 121305 0 None 97 2 Human 7.6 pKi = 7.6 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 297 5 1 3 3.2 Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
10430935 112571 1 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 397 10 1 2 6.0 Fc1ccc(C(SCCNCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b01373
CHEMBL3126735 112571 1 None 2 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 397 10 1 2 6.0 Fc1ccc(C(SCCNCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.6b01373
CHEMBL5282085 200921 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 0 5 3.1 Cn1ncc2cc(CN3CCO[C@H](COc4ccc(F)c(F)c4)C3)ccc21 10.1016/j.ejmech.2022.114840
155536720 178966 0 None 77 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4473652 178966 0 None 77 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 359 4 1 3 3.9 Cc1cccc(NC(=O)CN2CCN(c3cccc4ccccc34)CC2)c1 10.1021/acs.jmedchem.9b00231
135398737 7745 93 None -13 90 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
38 7745 93 None -13 90 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
722 7745 93 None -13 90 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
CHEMBL42 7745 93 None -13 90 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
DB00363 7745 93 None -13 90 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
57399432 77240 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946254 77240 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
57399432 77240 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL1946254 77240 0 None 2 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 4 5.5 Clc1ccc(N2CCCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
137635734 162891 0 None 61 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4063176 162891 0 None 61 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 377 7 0 3 3.2 O=C1CCc2ccccc2N1CCCN1CCN(CCc2ccccc2)CC1 10.1021/acs.jmedchem.8b00265
44336552 118117 1 None 18 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL326864 118117 1 None 18 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
10573099 214607 0 None -6 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 400 9 0 4 4.9 COc1cccc(C(=O)CCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL96322 214607 0 None -6 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 400 9 0 4 4.9 COc1cccc(C(=O)CCCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
164628883 193230 0 None -14 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4876546 193230 0 None -14 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
11652518 172711 0 None 16 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4cccnc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL425064 172711 0 None 16 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4cccnc4n3)CC2)cc1 10.1021/jm060166w
16277250 117269 4 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC(C(=O)N1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL324867 117269 4 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC(C(=O)N1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44426510 92519 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL229025 92519 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
134153539 161284 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3971383 161284 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990611 161284 0 None -6 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 390 5 0 3 6.0 Clc1ccc2sc(CCCCN3CCc4c(Cl)cccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
11384207 90127 0 None -165 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm0611152
CHEMBL219274 90127 0 None -165 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm0611152
11569619 143341 0 None -66 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 500 9 1 6 4.3 Cc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL373873 143341 0 None -66 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 500 9 1 6 4.3 Cc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
11670421 175574 0 None -10 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 492 11 1 8 3.0 COc1ccc(Cn2nnc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
CHEMBL437525 175574 0 None -10 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 492 11 1 8 3.0 COc1ccc(Cn2nnc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2C)cc1 10.1021/jm0611152
90644072 118816 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 340 4 0 3 4.5 Clc1ccc(N2CCN(CCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289652 118816 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 340 4 0 3 4.5 Clc1ccc(N2CCN(CCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
44438186 153986 3 None -7 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccccc2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL392822 153986 3 None -7 3 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2ccccc2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
11016342 109581 0 None -186 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 481 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm020952a
CHEMBL305362 109581 0 None -186 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 481 8 1 3 6.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccc2)cc1 10.1021/jm020952a
76311262 113070 0 None -660 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 468 11 2 5 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133779 113070 0 None -660 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 468 11 2 5 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139053 113070 0 None -660 3 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 468 11 2 5 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
71061724 152330 0 None -2 5 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL3915107 152330 0 None -2 5 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
56664950 73399 2 None -11 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 9 1 6 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c(OC)c1 10.1016/j.bmc.2011.04.021
CHEMBL1813592 73399 2 None -11 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 9 1 6 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c(OC)c1 10.1016/j.bmc.2011.04.021
CHEMBL1852737 73399 2 None -11 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 9 1 6 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)c(OC)c1 10.1016/j.bmc.2011.04.021
155195311 181126 0 None -208 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4551160 181126 0 None -208 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
44330554 215001 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL98578 215001 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 2.9 Cc1sc(C)c2c1CCc1cn(C)nc1-2 10.1016/s0960-894x(03)00587-0
17756102 92919 0 None -123 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL231171 92919 0 None -123 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
11512263 91142 0 None -89 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 544 11 1 7 4.7 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2C)cc1 10.1021/jm0611152
CHEMBL221866 91142 0 None -89 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 544 11 1 7 4.7 COc1ccc(Cn2nnc(C(=O)NCCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2C)cc1 10.1021/jm0611152
154726529 183224 1 None -26 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4467486 183224 1 None -26 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596338 183224 1 None -26 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
10469437 63315 1 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 289 1 0 2 4.6 CN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL163863 63315 1 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 289 1 0 2 4.6 CN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
135398737 7745 93 None -7 90 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 7745 93 None -7 90 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 7745 93 None -7 90 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 7745 93 None -7 90 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 7745 93 None -7 90 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]YM-09151 towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
30740059 114445 1 None 2 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 409 6 0 5 2.8 COc1ccc(OC)c(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)c1 10.1016/s0960-894x(02)00656-x
CHEMBL319043 114445 1 None 2 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 409 6 0 5 2.8 COc1ccc(OC)c(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)c1 10.1016/s0960-894x(02)00656-x
135398745 9688 112 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
47 9688 112 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
CHEMBL715 9688 112 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
DB00334 9688 112 None -10 65 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4.2 in CHO cellsBinding affinity towards human Dopamine receptor D4.2 in CHO cells
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm960268u
44335813 12131 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106914 12131 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00655-8
127030612 146108 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792725 146108 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 5 0 4 3.7 Clc1ccc(CN2CCO[C@H](COc3cccc(Cl)n3)C2)cc1 10.1016/j.bmcl.2016.03.102
10115074 127452 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 453 4 0 4 4.1 COc1ccc(Cl)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
CHEMBL354699 127452 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 453 4 0 4 4.1 COc1ccc(Cl)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
25070416 118562 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nn2ccccc12 10.1021/jm5004039
CHEMBL3287401 118562 0 None -4 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1c(OCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)nn2ccccc12 10.1021/jm5004039
44426508 92517 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.8 CC(c1ccccc1)N1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.096
CHEMBL229023 92517 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.8 CC(c1ccccc1)N1CCC(NC(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2006.12.096
118709174 120199 0 None -10 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 946 23 0 10 9.6 CN(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)CCN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318847 120199 0 None -10 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 946 23 0 10 9.6 CN(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)CCN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10641637 125558 0 None 19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)cc4)CC3)c2c1 10.1021/jm0009989
CHEMBL342001 125558 0 None 19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)cc4)CC3)c2c1 10.1021/jm0009989
11290928 12078 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 6 0 3 4.2 COc1ccccc1CCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL106665 12078 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 345 6 0 3 4.2 COc1ccccc1CCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
44372198 55914 0 None 199 4 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 420 4 0 4 5.1 Fc1ccc(-c2cccc3c(CN4CCN(c5ccc(Cl)cc5)CC4)cnn23)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL156198 55914 0 None 199 4 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 420 4 0 4 5.1 Fc1ccc(-c2cccc3c(CN4CCN(c5ccc(Cl)cc5)CC4)cnn23)cc1 10.1016/s0960-894x(01)00814-9
162671033 190534 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4793296 190534 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803797 190534 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
44264622 103918 4 None 22 4 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 327 3 0 5 2.7 Clc1ccc(N2CCN(Cc3cnc4ncccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL267853 103918 4 None 22 4 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 327 3 0 5 2.7 Clc1ccc(N2CCN(Cc3cnc4ncccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
122177644 127990 0 None -239 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577345 127990 0 None -239 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
44335569 11931 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2Cl)CCO1 10.1021/jm031111m
CHEMBL105894 11931 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 395 7 0 4 4.7 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2Cl)CCO1 10.1021/jm031111m
44319370 113824 0 None 1 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
CHEMBL315564 113824 0 None 1 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
13014680 105221 1 None -407 4 Human 5.5 pKi = 5.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL275696 105221 1 None -407 4 Human 5.5 pKi = 5.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 324 1 0 2 4.0 CN1CCN(C2=Cc3cc(Cl)ccc3Cc3ccccc32)CC1 10.1021/jm00043a008
1499 8872 47 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
3779 8872 47 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
536 8872 47 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
CHEMBL434 8872 47 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
DB01064 8872 47 None -18 17 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2016.04.028
71462266 88606 0 None -34 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1ccc2ccccc2c1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164355 88606 0 None -34 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 433 6 0 3 5.7 O=C(c1ccc2ccccc2c1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
154706513 183365 1 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4440698 183365 1 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4597532 183365 1 None -4 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
10803829 18377 1 None -288 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL1180636 18377 1 None -288 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL135725 18377 1 None -288 5 Human 6.5 pKi = 6.5 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
57587922 178291 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 235 3 1 4 1.8 CCCN1CC(c2ccc(N)nc2)OC[C@@H]1C 10.1021/acs.jmedchem.9b00702
CHEMBL4464060 178291 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 235 3 1 4 1.8 CCCN1CC(c2ccc(N)nc2)OC[C@@H]1C 10.1021/acs.jmedchem.9b00702
CHEMBL5077114 221261 0 None -2137 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
155195486 176466 0 None -14 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4437740 176466 0 None -14 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
16094677 90111 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
CHEMBL219185 90111 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 325 4 1 3 2.4 Cc1cccc(NC(=O)CN2CCC(c3cccc[n+]3[O-])CC2)c1 10.1021/jm060662k
9929629 108893 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 377 4 0 3 3.5 CCN1C(=O)C(N2CCN(Cc3ccc(C)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL302340 108893 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 377 4 0 3 3.5 CCN1C(=O)C(N2CCN(Cc3ccc(C)cc3)CC2)CCc2ccccc21 10.1016/s0960-894x(00)00421-2
44332581 11153 0 None -6 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccccc1OCCNCc1ccccc1 10.1016/s0960-894x(98)00014-6
CHEMBL101285 11153 0 None -6 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1ccccc1OCCNCc1ccccc1 10.1016/s0960-894x(98)00014-6
71658075 97176 0 None -194 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 437 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386614 97176 0 None -194 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 437 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1016/j.bmc.2013.03.074
109030343 177639 1 None 15 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 177639 1 None 15 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
122180568 128498 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588913 128498 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 441 8 0 6 4.6 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4ccccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
163322331 198994 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5204764 198994 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
44431492 95051 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2ccccn2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234827 95051 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2ccccn2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
11637457 79862 1 None -8 5 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
CHEMBL201093 79862 1 None -8 5 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
163322331 198994 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5204764 198994 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
44438230 100332 3 None -194 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246439 100332 3 None -194 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
10021193 73137 0 None 199 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL185156 73137 0 None 199 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.07.045
44214766 73839 0 None 275 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL187236 73839 0 None 275 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
11559589 129485 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL360424 129485 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2004.07.045
72901200 126555 25 None 154 4 Human 8.5 pKi = 8.5 Binding
Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5210307
CHEMBL3480577 126555 25 None 154 4 Human 8.5 pKi = 8.5 Binding
Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4Affinity Biochemical interaction (Radioligand binding assay) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5210307
9995379 113727 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
CHEMBL314952 113727 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
135887940 18107 0 None 93 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 1 6 2.9 COc1ccccc1N1CCN(CCCNC2=Nc3ccccc3OC2)CC1 10.1016/S0960-894X(97)00442-3
CHEMBL1179506 18107 0 None 93 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 1 6 2.9 COc1ccccc1N1CCN(CCCNC2=Nc3ccccc3OC2)CC1 10.1016/S0960-894X(97)00442-3
CHEMBL80711 18107 0 None 93 2 Human 8.5 pKi = 8.5 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 1 6 2.9 COc1ccccc1N1CCN(CCCNC2=Nc3ccccc3OC2)CC1 10.1016/S0960-894X(97)00442-3
44264642 211582 0 None 75 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7506 211582 0 None 75 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
10454684 211584 0 None 467 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 418 3 0 4 3.3 Ic1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7508 211584 0 None 467 4 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 418 3 0 4 3.3 Ic1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
9909648 212352 3 None -1 11 Rat 8.5 pKi = 8.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL81330 212352 3 None -1 11 Rat 8.5 pKi = 8.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
9995379 113727 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
CHEMBL314952 113727 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 307 3 1 3 2.5 O=C1Cc2c(cccc2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
10836365 214042 0 None 16 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 429 7 2 4 3.9 COc1cc(NC(=O)C(C)C)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL93021 214042 0 None 16 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 429 7 2 4 3.9 COc1cc(NC(=O)C(C)C)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
231915 98933 7 None 14 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 296 5 0 3 3.4 CCOc1ccccc1N1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420892 98933 7 None 14 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 296 5 0 3 3.4 CCOc1ccccc1N1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.07.033
10220333 10979 0 None 36 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 236 0 0 4 3.4 Cc1sc(C)c2c1SCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
CHEMBL100203 10979 0 None 36 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 236 0 0 4 3.4 Cc1sc(C)c2c1SCc1cnn(C)c1-2 10.1016/s0960-894x(03)00587-0
44336030 11983 0 None 251 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL106169 11983 0 None 251 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
10001810 12113 0 None 91 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1cc(Cl)ccc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL106862 12113 0 None 91 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1cc(Cl)ccc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
44335919 115705 0 None 31 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.5 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL321121 115705 0 None 31 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 377 5 0 3 3.5 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
1946142 116398 2 None 478 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 393 4 0 5 2.5 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL322222 116398 2 None 478 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 393 4 0 5 2.5 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1016/s0960-894x(02)00656-x
44335739 11619 0 None 7 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 380 4 0 2 4.7 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1F 10.1016/s0960-894x(02)00655-8
CHEMBL104273 11619 0 None 7 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 380 4 0 2 4.7 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1F 10.1016/s0960-894x(02)00655-8
9799123 12391 0 None 35 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL107742 12391 0 None 35 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44336006 13023 0 None 398 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 5 0 5 3.5 O=c1sc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL108157 13023 0 None 398 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 5 0 5 3.5 O=c1sc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
72901200 126555 25 None 154 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.1016/j.ejmech.2020.113141
CHEMBL3480577 126555 25 None 154 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.1016/j.ejmech.2020.113141
9909648 212352 3 None 1 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-nemonapride from human D4 receptor assessed as inhibition constantDisplacement of [3H]-nemonapride from human D4 receptor assessed as inhibition constant
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1016/j.ejmech.2020.113141
CHEMBL81330 212352 3 None 1 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-nemonapride from human D4 receptor assessed as inhibition constantDisplacement of [3H]-nemonapride from human D4 receptor assessed as inhibition constant
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1016/j.ejmech.2020.113141
54581963 68375 0 None -11 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 437 8 0 5 3.7 COc1ccc2c(c1)CCCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
CHEMBL1771105 68375 0 None -11 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 437 8 0 5 3.7 COc1ccc2c(c1)CCCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
11559589 129485 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL360424 129485 0 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@H]1CCN(Cc2ccccc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
135921193 46968 0 None 93 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 366 5 1 6 2.5 COc1ccccc1N1CCN(CCNC2=Nc3ccccc3OC2)CC1 10.1021/jm981041x
CHEMBL148024 46968 0 None 93 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 366 5 1 6 2.5 COc1ccccc1N1CCN(CCNC2=Nc3ccccc3OC2)CC1 10.1021/jm981041x
9909648 212352 3 None 1 11 Human 8.5 pKi = 8.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL81330 212352 3 None 1 11 Human 8.5 pKi = 8.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.7b00151
10684706 92497 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL22892 92497 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10617366 212221 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 343 5 1 2 4.7 Cc1c(-c2ccccc2)n[nH]c1C1=CCN(CCc2ccccc2)CC1 10.1021/jm970111h
CHEMBL80318 212221 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 343 5 1 2 4.7 Cc1c(-c2ccccc2)n[nH]c1C1=CCN(CCc2ccccc2)CC1 10.1021/jm970111h
10404144 212081 23 None 1 10 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL7927 212081 23 None 1 10 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
10980338 174787 0 None 1584 4 Human 8.5 pKi = 8.5 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3ccc4ccnn4c3)CC2)cc1 10.1021/jm015522j
CHEMBL432059 174787 0 None 1584 4 Human 8.5 pKi = 8.5 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3ccc4ccnn4c3)CC2)cc1 10.1021/jm015522j
10336538 8406 50 None -3 8 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2013.07.033
974 8406 50 None -3 8 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2013.07.033
CHEMBL310843 8406 50 None -3 8 Human 8.5 pKi = 8.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2013.07.033
10684706 92497 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL22892 92497 0 None 75 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 287 9 2 4 2.8 Oc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
11003833 51537 0 None 2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 397 9 1 5 3.0 COc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL152159 51537 0 None 2 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 397 9 1 5 3.0 COc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
10404144 212081 23 None 1 10 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/j.ejmech.2020.113141
CHEMBL7927 212081 23 None 1 10 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/j.ejmech.2020.113141
10404144 212081 23 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL7927 212081 23 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/j.bmc.2014.04.026
21219164 98325 0 None 120 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL24051 98325 0 None 120 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(99)00169-9
12052258 106870 0 None 4 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1nn(C2CCN(Cc3cccc(Cl)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL287412 106870 0 None 4 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 4 0 3 5.3 Cc1nn(C2CCN(Cc3cccc(Cl)c3)CC2)cc1-c1ccccc1 10.1016/s0960-894x(99)00169-9
10404144 212081 23 None 1 10 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL7927 212081 23 None 1 10 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
9840672 213096 0 None -5 4 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 335 6 2 3 3.8 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL87192 213096 0 None -5 4 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 335 6 2 3 3.8 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
2780 117306 36 None -4 10 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00678-4
CHEMBL325109 117306 36 None -4 10 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00678-4
44412458 146072 3 None 28 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 316 4 0 4 3.6 C1=C(c2ccccc2)CCN(Cc2cn(-c3ccccc3)nn2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL379177 146072 3 None 28 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 316 4 0 4 3.6 C1=C(c2ccccc2)CCN(Cc2cn(-c3ccccc3)nn2)C1 10.1016/j.bmcl.2006.02.075
9821010 62229 0 None 575 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 4 0 4 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(Cl)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL161982 62229 0 None 575 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 4 0 4 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(Cl)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44419066 91137 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.6 c1ccc(C2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1021/jm0611152
CHEMBL221814 91137 0 None 28 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 318 4 0 4 3.6 c1ccc(C2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1021/jm0611152
44340227 117418 0 None 16 4 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325772 117418 0 None 16 4 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
10574818 214680 0 None 9 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 7 2 4 4.1 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCCCC2)C1 10.1021/jm9601720
CHEMBL96703 214680 0 None 9 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 433 7 2 4 4.1 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CC2CCCCC2)C1 10.1021/jm9601720
1353 8692 93 None -3 85 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
3559 8692 93 None -3 85 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
86 8692 93 None -3 85 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
CHEMBL54 8692 93 None -3 85 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
DB00502 8692 93 None -3 85 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
9948461 26273 1 None 5 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 269 9 1 2 3.7 c1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL129931 26273 1 None 5 3 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 269 9 1 2 3.7 c1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
155532505 178537 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 10 2 5 5.0 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4467437 178537 0 None 9 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 569 10 2 5 5.0 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
127028185 146114 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792751 146114 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 375 5 1 4 3.6 Fc1ccc2c(CN3CCO[C@H](COc4cccc(Cl)n4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
127032383 146181 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL3793438 146181 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.ejmech.2022.114840
54580906 68379 0 None -15 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771109 68379 0 None -15 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53363109 70622 0 None 19 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 465 11 0 8 4.0 CCCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803030 70622 0 None 19 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 465 11 0 8 4.0 CCCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
1353 8692 93 None -3 85 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
3559 8692 93 None -3 85 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
86 8692 93 None -3 85 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
CHEMBL54 8692 93 None -3 85 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
DB00502 8692 93 None -3 85 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00108-5
22065997 106131 0 None 64 4 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
CHEMBL282424 106131 0 None 64 4 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 310 3 1 3 3.0 Fc1ccccc1N1CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/s0960-894x(01)00241-4
44400500 172839 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
CHEMBL425731 172839 0 None -1 5 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm050170s
127032383 146181 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.ejmech.2022.114840
CHEMBL3793438 146181 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3ccc4[nH]ccc4c3)CCO2)cc1 10.1016/j.ejmech.2022.114840
10593191 195887 1 None 33 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL51023 195887 1 None 33 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
44394667 73813 0 None 27 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL187113 73813 0 None 27 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 362 5 1 3 4.4 O=C(N[C@@H]1CCN(Cc2ccccc2)C1)c1cccc(-c2ccsc2)c1 10.1016/j.bmcl.2004.07.045
10741841 213859 0 None 23 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 8 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CCc2ccccc2)C1 10.1021/jm9601720
CHEMBL91859 213859 0 None 23 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 8 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(CCc2ccccc2)C1 10.1021/jm9601720
977 7961 5 None -10 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human D4R assessed as inhibition constantBinding affinity to human D4R assessed as inhibition constant
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/j.ejmech.2020.113141
9820261 7961 5 None -10 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human D4R assessed as inhibition constantBinding affinity to human D4R assessed as inhibition constant
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/j.ejmech.2020.113141
CHEMBL66227 7961 5 None -10 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to human D4R assessed as inhibition constantBinding affinity to human D4R assessed as inhibition constant
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/j.ejmech.2020.113141
155513773 176603 0 None 12 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 551 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4439644 176603 0 None 12 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 551 10 2 5 4.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.9b01085
54580905 68377 0 None -13 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771107 68377 0 None -13 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53327908 68383 0 None -28 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 470 8 0 5 4.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccncc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771112 68383 0 None -28 5 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 470 8 0 5 4.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccncc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
10594054 38187 1 None 97 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2cc(CN3CCN(c4ccccc4Cl)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL140258 38187 1 None 97 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2cc(CN3CCN(c4ccccc4Cl)CC3)[nH]c2c1 10.1021/jm0009989
45268292 203466 0 None 138 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 460 4 1 6 3.5 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL564688 203466 0 None 138 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 460 4 1 6 3.5 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
977 7961 5 None -10 4 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/s0960-894x(98)00108-5
9820261 7961 5 None -10 4 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/s0960-894x(98)00108-5
CHEMBL66227 7961 5 None -10 4 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 10.1016/s0960-894x(98)00108-5
10473658 193972 3 None 38 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49231 193972 3 None 38 3 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 359 5 1 4 2.9 COc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
133008 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm970111h
3302 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm970111h
CHEMBL444309 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm970111h
133008 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm991029k
3302 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm991029k
CHEMBL444309 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm991029k
1524 8962 96 None -4 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
197 8962 96 None -4 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
3822 8962 96 None -4 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
88 8962 96 None -4 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
CHEMBL51 8962 96 None -4 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
DB12465 8962 96 None -4 51 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm0002432
133008 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm0002432
3302 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm0002432
CHEMBL444309 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm0002432
44209480 76945 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL1940418 76945 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2020.115943
133008 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1016/j.ejmech.2020.113141
3302 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1016/j.ejmech.2020.113141
CHEMBL444309 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1016/j.ejmech.2020.113141
134135650 151144 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 372 5 1 1 5.4 Fc1ccc2c(CN3CCC(F)(F)[C@H](CCc4ccccc4)C3)c[nH]c2c1 10.1016/j.ejmech.2022.114840
CHEMBL3905761 151144 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 372 5 1 1 5.4 Fc1ccc2c(CN3CCC(F)(F)[C@H](CCc4ccccc4)C3)c[nH]c2c1 10.1016/j.ejmech.2022.114840
44209480 76945 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL1940418 76945 0 None -3 11 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
44209480 76945 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940418 76945 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
44209480 76945 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940418 76945 0 None -3 11 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
133008 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm960072u
3302 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm960072u
CHEMBL444309 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 10.1021/jm960072u
15817410 64309 0 None 331 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL166269 64309 0 None 331 2 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
134135650 151144 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 372 5 1 1 5.4 Fc1ccc2c(CN3CCC(F)(F)[C@H](CCc4ccccc4)C3)c[nH]c2c1 10.1016/j.ejmech.2022.114840
CHEMBL3905761 151144 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 372 5 1 1 5.4 Fc1ccc2c(CN3CCC(F)(F)[C@H](CCc4ccccc4)C3)c[nH]c2c1 10.1016/j.ejmech.2022.114840
168275783 199606 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc([N+](=O)[O-])c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5176100 199606 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc([N+](=O)[O-])c2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221583 199606 0 None 354 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2cccc([N+](=O)[O-])c2)CC1 10.1021/acs.jmedchem.2c00840
9995264 213962 0 None 93 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 305 2 0 3 3.7 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
CHEMBL92489 213962 0 None 93 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 305 2 0 3 3.7 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1021/jm970170v
10691599 209368 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm970111h
CHEMBL61195 209368 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm970111h
44278788 117115 1 None 147 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 OC(COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL32402 117115 1 None 147 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 327 7 1 4 3.0 OC(COc1ccccc1)CN1CCC(Oc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10404144 212081 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm015522j
CHEMBL7927 212081 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm015522j
10404144 212081 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm049612a
CHEMBL7927 212081 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm049612a
CHEMBL146246 45052 0 None 1 9 Human 8.4 pKi = 8.4 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1016/j.ejmech.2020.113141
9995264 213962 0 None 93 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 305 2 0 3 3.7 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL92489 213962 0 None 93 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 305 2 0 3 3.7 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
9906978 49485 2 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL150161 49485 2 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
9906978 49485 2 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL150161 49485 2 None 1 12 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
973 7960 39 None -9 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human D4.4 receptorBinding affinity towards human D4.4 receptor
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
9796720 7960 39 None -9 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human D4.4 receptorBinding affinity towards human D4.4 receptor
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
CHEMBL77395 7960 39 None -9 6 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human D4.4 receptorBinding affinity towards human D4.4 receptor
ChEMBL 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 10.1021/jm030505a
188942 9594 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
3297 9594 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
979 9594 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
CHEMBL103772 9594 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm0002432
155515931 176790 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442470 176790 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2F)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
1353 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
3559 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
86 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
CHEMBL54 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
DB00502 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00218-7
10691599 209368 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm960072u
CHEMBL61195 209368 0 None 22 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)no3)CC2)cc1 10.1021/jm960072u
10567430 126071 1 None 851 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2cc(CN3CCN(c4ccccc4)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL343880 126071 1 None 851 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2cc(CN3CCN(c4ccccc4)CC3)[nH]c2c1 10.1021/jm0009989
10404144 212081 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm060166w
CHEMBL7927 212081 23 None 1 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm060166w
9905249 106678 0 None -2 3 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28607 106678 0 None -2 3 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 322 4 1 4 2.9 COc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
133079 10410 42 None 1 3 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/acs.jmedchem.7b00151
980 10410 42 None 1 3 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL69759 10410 42 None 1 3 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/acs.jmedchem.7b00151
44454734 104503 0 None 20 5 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2ccc(OCCF)cc2)CC1 10.1016/j.bmcl.2007.12.026
CHEMBL271513 104503 0 None 20 5 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2ccc(OCCF)cc2)CC1 10.1016/j.bmcl.2007.12.026
3303 9024 46 None -1 15 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
5311200 9024 46 None -1 15 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
CHEMBL267014 9024 46 None -1 15 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00241-4
10545941 45699 0 None 181 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL146757 45699 0 None 181 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
188942 9594 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
3297 9594 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
979 9594 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
CHEMBL103772 9594 41 None -12 4 Human 8.4 pKi = 8.4 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 10.1021/jm960637m
44326212 214207 0 None 37 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 459 6 2 4 4.5 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CCCC2CCC3)C1 10.1021/jm9601720
CHEMBL94050 214207 0 None 37 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 459 6 2 4 4.5 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CCCC2CCC3)C1 10.1021/jm9601720
155512259 176427 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2cccc(F)c2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4437233 176427 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2cccc(F)c2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
132060812 168815 0 None 16 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4160064 168815 0 None 16 10 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 329 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CCN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
71450707 90853 0 None 15 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207640 90853 0 None 15 7 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
45273443 202410 0 None 66 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.2 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL556288 202410 0 None 66 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 392 4 1 6 2.2 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
21997225 62557 0 None 48 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OCC2CCC3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL162265 62557 0 None 48 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OCC2CCC3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
11738728 25271 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
CHEMBL127290 25271 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assayIn vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay
ChEMBL 320 3 1 3 3.5 Cc1ccc(C)c(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm030505a
9817774 118274 0 None -5 4 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 299 6 3 4 3.0 Sc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL327782 118274 0 None -5 4 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 299 6 3 4 3.0 Sc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
1353 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
3559 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
86 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
CHEMBL54 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
DB00502 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/S0960-894X(97)00194-7
10760638 194955 0 None 131 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49876 194955 0 None 131 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
56852956 118820 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 118820 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
10425969 107785 3 None 346 4 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL294459 107785 3 None 346 4 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
792460 98921 7 None 28 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 302 5 0 4 3.5 CCOc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420773 98921 7 None 28 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 302 5 0 4 3.5 CCOc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
56852956 118820 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289656 118820 1 None 10 9 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 339 5 0 6 2.8 c1cnc(N2CCN(CCCc3nc4ccccc4s3)CC2)nc1 10.1016/j.bmc.2014.04.026
137634397 162884 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4063145 162884 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
10069973 59173 0 None -4 4 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 407 9 0 6 4.4 COc1ccccc1C(=O)CCCCCN1CCN(c2noc3ccccc23)CC1 10.1021/jm020994z
CHEMBL159022 59173 0 None -4 4 Human 8.4 pKi = 8.4 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 407 9 0 6 4.4 COc1ccccc1C(=O)CCCCCN1CCN(c2noc3ccccc23)CC1 10.1021/jm020994z
44369020 126237 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm020952a
CHEMBL345111 126237 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 374 6 1 5 2.3 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/jm020952a
10425450 6989 30 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 6989 30 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 6989 30 None -1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
17461770 208619 1 None 10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 360 5 1 3 3.9 COc1cc2ccccc2cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
CHEMBL60708 208619 1 None 10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 360 5 1 3 3.9 COc1cc2ccccc2cc1C(=O)NC1CCN(Cc2ccccc2)C1 10.1021/jm960017l
44370032 54163 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.4 C1=C(/C=C/c2ccccc2)CCN(CCc2cc3ccc[nH]c-3n2)C1 10.1016/s0960-894x(99)00025-6
CHEMBL154482 54163 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.4 C1=C(/C=C/c2ccccc2)CCN(CCc2cc3ccc[nH]c-3n2)C1 10.1016/s0960-894x(99)00025-6
10092819 23545 0 None -28 11 Human 7.5 pKi = 7.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm049612a
CHEMBL124444 23545 0 None -28 11 Human 7.5 pKi = 7.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm049612a
10092819 23545 0 None -28 11 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
CHEMBL124444 23545 0 None -28 11 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
11068912 37637 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL139722 37637 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
10542345 25652 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128281 25652 0 None 7 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 9 1 3 4.1 Cc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
135398737 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
38 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
722 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
CHEMBL42 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
DB00363 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020952a
10781960 22331 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2cc(CN3CCN(c4ccccc4)CC3)ccc2o1 10.1021/jm990266k
CHEMBL121993 22331 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 320 3 0 4 3.1 O=c1ccc2cc(CN3CCN(c4ccccc4)CC3)ccc2o1 10.1021/jm990266k
162671033 190534 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4793296 190534 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4803797 190534 0 None 3 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2cccnc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
154726793 183012 1 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4590966 183012 1 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594692 183012 1 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
135398737 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
38 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
722 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
CHEMBL42 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
DB00363 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm020938y
2726 7706 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
621 7706 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
83 7706 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
CHEMBL71 7706 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
DB00477 7706 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
49782602 23941 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 583 6 1 3 7.4 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256169 23941 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 583 6 1 3 7.4 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
49782604 24295 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 379 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1257927 24295 0 None 1 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 379 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
137636351 162652 0 None -87 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4060403 162652 0 None -87 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
73347474 97834 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
CHEMBL2397478 97834 0 None -30 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
71733935 97758 0 None -43 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2396663 97758 0 None -43 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
122177641 127987 0 None -47 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577342 127987 0 None -47 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
11474021 11566 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 365 6 0 4 3.8 COc1ccc(F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104089 11566 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 365 6 0 4 3.8 COc1ccc(F)cc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
135398737 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
38 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
722 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
CHEMBL42 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
DB00363 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991138z
53248675 73143 0 None -213 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 407 8 1 5 3.5 COc1ccccc1N1CCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813594 73143 0 None -213 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 407 8 1 5 3.5 COc1ccccc1N1CCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1851639 73143 0 None -213 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 407 8 1 5 3.5 COc1ccccc1N1CCN(CCCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
168293632 199779 0 None 27 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 1 3 3.3 c1ccc(N2CCN(CCCc3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5203856 199779 0 None 27 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 1 3 3.3 c1ccc(N2CCN(CCCc3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5222695 199779 0 None 27 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 320 5 1 3 3.3 c1ccc(N2CCN(CCCc3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.2c00840
10092819 23545 0 None -28 11 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0611152
CHEMBL124444 23545 0 None -28 11 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0611152
11068912 37637 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL139722 37637 0 None 8 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
135398737 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
38 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
722 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
CHEMBL42 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
DB00363 7745 93 None -13 90 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.07.068
90644068 118814 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 369 6 0 4 4.6 Clc1ccc(N2CCN(CCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289650 118814 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 369 6 0 4 4.6 Clc1ccc(N2CCN(CCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
10616050 193425 3 None 81 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL48807 193425 3 None 81 3 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 325 5 1 4 2.2 COc1ccccc1N1CCN(CNC(=O)c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
164621627 192262 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4862180 192262 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
44419053 91062 0 None -79 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2sc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm0611152
CHEMBL221397 91062 0 None -79 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 8 1 5 4.2 C#Cc1ccc2sc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2c1 10.1021/jm0611152
44323890 213696 0 None -4 4 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 316 1 0 2 4.2 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL90977 213696 0 None -4 4 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 316 1 0 2 4.2 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
49783039 24425 0 None -120 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 421 7 1 4 4.9 Cc1ccc(C)c(N2CCN(CCCCNC(=O)c3cc4ccccc4s3)CC2)c1 10.1021/jm100899z
CHEMBL1258383 24425 0 None -120 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 421 7 1 4 4.9 Cc1ccc(C)c(N2CCN(CCCCNC(=O)c3cc4ccccc4s3)CC2)c1 10.1021/jm100899z
127045855 146442 0 None -3 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797876 146442 0 None -3 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
118709163 120186 0 None -112 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 888 21 0 8 11.3 O=C(CCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318835 120186 0 None -112 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 888 21 0 8 11.3 O=C(CCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137655795 165361 0 None -120 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4091933 165361 0 None -120 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
3038495 7495 37 None -91 18 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
7625 7495 37 None -91 18 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
CHEMBL25236 7495 37 None -91 18 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]YM-09151-2 binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
10917920 118223 0 None -3801 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL327527 118223 0 None -3801 10 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
10404663 173640 10 None -100 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 334 9 1 3 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL428561 173640 10 None -100 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 334 9 1 3 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)ccc1OC 10.1016/j.bmc.2007.07.017
122189390 130023 0 None -323 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613876 130023 0 None -323 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
25129807 110071 0 None -154 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
CHEMBL3084502 110071 0 None -154 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1016/j.bmc.2008.12.054
44330640 215080 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 3.0 Cc1sc(C)c2c1CCCc1nccn1-2 10.1016/s0960-894x(03)00587-0
CHEMBL99054 215080 1 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 218 0 0 3 3.0 Cc1sc(C)c2c1CCCc1nccn1-2 10.1016/s0960-894x(03)00587-0
164619170 192380 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 192380 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
168271259 197294 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5179459 197294 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
163322331 198994 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5204764 198994 3 None 8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 408 6 1 3 4.5 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(F)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
11720119 90001 0 None -27 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 490 12 1 7 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
CHEMBL218607 90001 0 None -27 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 490 12 1 7 3.6 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1 10.1021/jm0611152
164619170 192380 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 192380 0 None -45 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
9888555 172383 16 None -208 8 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL424294 172383 16 None -208 8 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
130431334 181205 0 None -1513 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CCC(O)CNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4552939 181205 0 None -1513 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CCC(O)CNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
168271259 197294 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5179459 197294 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
168271259 197294 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179459 197294 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cc1nc(CN2CCC(OCc3cccc(C(F)(F)F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
53248159 68763 0 None -501 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
CHEMBL1774384 68763 0 None -501 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 500 8 1 4 5.3 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm200288r
10098342 144768 0 None -891 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 523 7 1 4 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2o1 10.1021/jm0611152
CHEMBL376445 144768 0 None -891 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 523 7 1 4 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2o1 10.1021/jm0611152
72164300 98930 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 370 3 0 2 5.5 Clc1cccc(N2CCN(Cc3cccc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420782 98930 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 370 3 0 2 5.5 Clc1cccc(N2CCN(Cc3cccc4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
44393415 72004 0 None -12 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 499 8 1 5 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)s2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL182652 72004 0 None -12 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 499 8 1 5 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)s2)CC1 10.1016/j.bmcl.2004.05.052
44336352 117777 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.6 CCC1(CC)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL326250 117777 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.6 CCC1(CC)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
9818076 22996 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 7 2 4 3.4 O=c1ccc2ccc(CNCCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL122427 22996 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 308 7 2 4 3.4 O=c1ccc2ccc(CNCCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL5286175 201116 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 340 1 1 4 4.0 Clc1ccc2c(c1)N=C(N1CCN(c3ccccc3)CC1)CCN2 10.1016/j.ejmech.2020.113141
164621627 192262 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4862180 192262 0 None -13 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 369 5 0 4 3.7 O=C1c2ccc(Cl)cc2CC1CCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
60167166 82070 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL2037430 82070 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
60167166 82070 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL2037430 82070 0 None 1 8 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
44431487 94849 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL234646 94849 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 374 5 1 3 4.2 COc1ccc(CN2CCC(NC(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/j.bmcl.2006.12.106
137632761 163353 0 None -13 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
CHEMBL4068561 163353 0 None -13 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 476 8 3 9 2.7 O=c1ccc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
137654675 165413 0 None -8 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4092441 165413 0 None -8 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
137633705 163397 0 None -57 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4069091 163397 0 None -57 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
122181331 128650 0 None -15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590082 128650 0 None -15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 414 9 1 3 5.4 CCCN(CCCCNC(=O)/N=N/c1ccc(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
10691634 107427 0 None 12 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.7 COc1cc2ccccc2cc1C(=O)CCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL292186 107427 0 None 12 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 387 7 0 3 5.7 COc1cc2ccccc2cc1C(=O)CCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
11793892 204830 0 None 31 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.3 COc1cc2ccccc2cc1COCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL57407 204830 0 None 31 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 375 7 0 3 5.3 COc1cc2ccccc2cc1COCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
44273912 84825 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20996 84825 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 8 1 3 3.8 CCCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44273897 105484 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 395 6 1 3 3.5 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL277669 105484 0 None 50 2 Human 7.5 pKi = 7.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 395 6 1 3 3.5 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(Br)cc2)CC1 10.1016/0960-894X(96)00198-9
2726 7706 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
621 7706 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
83 7706 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
CHEMBL71 7706 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
DB00477 7706 68 None -8 72 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]N-Methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2013.12.024
76325152 113148 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 113148 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 113148 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
53248677 73193 0 None -446 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 10 1 5 3.9 O=c1ccc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2[nH]1 10.1016/j.bmc.2011.04.021
CHEMBL1813595 73193 0 None -446 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 10 1 5 3.9 O=c1ccc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2[nH]1 10.1016/j.bmc.2011.04.021
CHEMBL1851893 73193 0 None -446 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 439 10 1 5 3.9 O=c1ccc2ccc(OCCCCN3CCN(c4ccccc4OCCF)CC3)cc2[nH]1 10.1016/j.bmc.2011.04.021
127053218 146256 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794336 146256 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 334 5 0 4 3.5 c1ccc(OC[C@@H]2CN(Cc3ccc4ccccc4n3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
17469721 84800 5 None 9 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 320 4 0 6 2.0 c1ccc(-n2cc(CN3CCN(c4ncccn4)CC3)cn2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL209832 84800 5 None 9 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 320 4 0 6 2.0 c1ccc(-n2cc(CN3CCN(c4ncccn4)CC3)cn2)cc1 10.1016/j.bmcl.2006.02.075
10359539 65828 10 None 41 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL169459 65828 10 None 41 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
3033769 10054 61 None -562 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
3299 10054 61 None -562 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
94 10054 61 None -562 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
CHEMBL8809 10054 61 None -562 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
DB12518 10054 61 None -562 18 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
25139180 191120 0 None -10 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
CHEMBL484357 191120 0 None -10 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
114840 76358 59 None 1 2 Human 5.5 pKi = 5.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 271 2 4 4 2.2 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1 10.1016/S0960-894X(97)00194-7
CHEMBL19344 76358 59 None 1 2 Human 5.5 pKi = 5.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 271 2 4 4 2.2 Oc1ccc(CC2NCCc3cc(O)c(O)cc32)cc1 10.1016/S0960-894X(97)00194-7
CHEMBL5079053 221380 0 None -107 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NCC2CCCN2CC(=O)N2CCC(c3ccccc3)(c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c00611
9926141 177035 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2cc(CNCCNc3ccccc3)ccc2o1 10.1021/jm990266k
CHEMBL444596 177035 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2cc(CNCCNc3ccccc3)ccc2o1 10.1021/jm990266k
11442138 75964 0 None 24 2 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
CHEMBL192650 75964 0 None 24 2 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@H]1CC2 10.1021/jm049031l
10470579 214153 0 None -16 4 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL93753 214153 0 None -16 4 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
155195487 180055 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4525362 180055 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
9816808 213089 0 None -51 4 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]ncc23)cc1 10.1016/s0960-894x(99)00434-5
CHEMBL87137 213089 0 None -51 4 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]ncc23)cc1 10.1016/s0960-894x(99)00434-5
49783419 24521 0 None -954 12 Rat 6.5 pKi = 6.5 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258671 24521 0 None -954 12 Rat 6.5 pKi = 6.5 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 366 6 1 6 2.8 CCCCN1CCC(COC(=O)c2cc(F)c(N)c3c2OCCO3)CC1 10.1021/jm100668r
130431277 176711 0 None -58 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4441358 176711 0 None -58 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl 10.1021/acs.jmedchem.6b00860
44376920 62129 0 None 3 2 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 381 5 1 6 2.4 CC(=O)Nc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL161899 62129 0 None 3 2 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 381 5 1 6 2.4 CC(=O)Nc1ccc(OC[C@@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
44273925 84069 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccc(N2CCN(CCCCNC(=O)C(C)(C)C)CC2)cc1 10.1016/0960-894X(96)00198-9
CHEMBL20819 84069 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 347 7 1 4 2.8 COc1ccc(N2CCN(CCCCNC(=O)C(C)(C)C)CC2)cc1 10.1016/0960-894X(96)00198-9
44273815 84910 2 None 2 2 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 317 6 1 3 2.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21035 84910 2 None 2 2 Human 6.5 pKi = 6.5 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 317 6 1 3 2.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2)CC1 10.1016/0960-894X(96)00198-9
168268918 196786 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.ejmech.2022.114840
CHEMBL5171398 196786 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.ejmech.2022.114840
137636308 162981 0 None 8 8 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4064222 162981 0 None 8 8 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 329 7 0 3 2.8 CCCCN1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
10430685 61073 0 None -107 4 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 393 8 1 6 4.1 O=C(CCCCCN1CCN(c2noc3ccccc23)CC1)c1ccccc1O 10.1021/jm020994z
CHEMBL160817 61073 0 None -107 4 Human 6.5 pKi = 6.5 Binding
Binding affinity of compound was tested for Dopamine receptor D4Binding affinity of compound was tested for Dopamine receptor D4
ChEMBL 393 8 1 6 4.1 O=C(CCCCCN1CCN(c2noc3ccccc23)CC1)c1ccccc1O 10.1021/jm020994z
6466372 176841 12 None 93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 176841 12 None 93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
53248256 68809 0 None -316 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 473 8 1 4 4.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm200288r
CHEMBL1774536 68809 0 None -316 4 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 473 8 1 4 4.5 COc1ccccc1N1CCN(CC(F)CCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm200288r
44438239 161713 2 None -13 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 352 4 2 3 4.4 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL401031 161713 2 None -13 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 352 4 2 3 4.4 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
168268918 196786 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.ejmech.2022.114840
CHEMBL5171398 196786 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.ejmech.2022.114840
168268918 196786 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
CHEMBL5171398 196786 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 369 5 1 3 4.7 Cc1cccc(CO[C@H]2CCCN(Cc3cc4ccc(Cl)cc4[nH]3)C2)n1 10.1016/j.bmcl.2022.128615
15290395 106675 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 3 4.7 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(F)cc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28605 106675 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 3 4.7 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(F)cc2)CC1 10.1016/S0960-894X(97)00233-3
44278829 107253 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 4 4.8 OC(COc1cccc2ccccc12)CN1CCC(Sc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL29087 107253 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 393 7 1 4 4.8 OC(COc1cccc2ccccc12)CN1CCC(Sc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
10065188 108381 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
CHEMBL298763 108381 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1021/jm970021c
135398737 7745 93 None -7 90 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 7745 93 None -7 90 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 7745 93 None -7 90 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 7745 93 None -7 90 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 7745 93 None -7 90 Rat 7.5 pKi = 7.5 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
2865 10915 73 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
59 10915 73 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
60854 10915 73 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL708 10915 73 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00246 10915 73 None -66 53 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
9905720 174712 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)c1 10.1021/jm990266k
CHEMBL431479 174712 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)c1 10.1021/jm990266k
10704110 122519 0 None -42 3 Human 7.5 pKi = 7.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 3 1 2 2.6 CCCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL335392 122519 0 None -42 3 Human 7.5 pKi = 7.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 3 1 2 2.6 CCCN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
16094699 88920 4 None 109 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
CHEMBL216794 88920 4 None 109 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]spiperone from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.0 Cc1cccc(C(=O)NCN2CCC(c3ccccn3)CC2)c1 10.1021/jm060662k
72544787 99905 0 None 6 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443008 99905 0 None 6 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
137644966 165273 0 None -45 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4091064 165273 0 None -45 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
21219160 98782 0 None 14 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 318 4 0 4 3.8 c1ccc(CN2CCC(n3cc(-c4ccccc4)nn3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL24170 98782 0 None 14 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 318 4 0 4 3.8 c1ccc(CN2CCC(n3cc(-c4ccccc4)nn3)CC2)cc1 10.1016/s0960-894x(99)00169-9
10014924 114048 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
CHEMBL316983 114048 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
10014924 114048 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
CHEMBL316983 114048 0 None -16 5 Human 7.5 pKi = 7.5 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
11383473 11652 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1ccccc1OCC1CN(Cc2ccc(Cl)c(Cl)c2)CCO1 10.1021/jm031111m
CHEMBL104431 11652 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1ccccc1OCC1CN(Cc2ccc(Cl)c(Cl)c2)CCO1 10.1021/jm031111m
11393899 11663 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104485 11663 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11360382 11816 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 359 7 0 3 4.6 CCCc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL105234 11816 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 359 7 0 3 4.6 CCCc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11795245 118480 0 None 25 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1cccc2c1CCCC2NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
CHEMBL2112375 118480 0 None 25 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1cccc2c1CCCC2NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
CHEMBL328681 118480 0 None 25 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1cccc2c1CCCC2NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
57394285 77233 0 None 5 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 378 6 0 3 5.2 Fc1ccc(SCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946125 77233 0 None 5 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 378 6 0 3 5.2 Fc1ccc(SCCCN2CCCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2012.01.022
11151920 86809 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212903 86809 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
76325152 113148 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 113148 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 113148 0 None -3 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
109030343 177639 1 None 15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 177639 1 None 15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10065188 108381 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL298763 108381 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 329 4 1 3 2.9 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccccc1 10.1016/j.bmcl.2005.02.012
49788940 25045 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 352 5 1 4 2.2 N#Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
CHEMBL1270422 25045 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 352 5 1 4 2.2 N#Cc1ccc(N2CCN(CCNC(=O)c3ccc(F)cc3)CC2)cc1 10.1021/jm100925m
10424961 213759 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL544184 213759 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
CHEMBL91350 213759 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00004a016
10424961 213759 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL544184 213759 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL91350 213759 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 CC1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL5283608 200999 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 345 6 0 6 3.0 CCOC(=O)c1nn(-c2ccccc2)cc1CN(C)[C@@H]1CCSC1 10.1016/j.ejmech.2020.113141
CHEMBL5280960 200869 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 336 5 0 5 3.2 Cc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)n1 10.1016/j.ejmech.2022.114840
9980998 37808 0 None -524 7 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 37808 0 None -524 7 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 37808 0 None -524 7 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
44538690 116628 0 None -354 7 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCO3)c1ccc(F)cc1 10.1021/jm401958n
CHEMBL3233432 116628 0 None -354 7 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 380 5 0 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCO3)c1ccc(F)cc1 10.1021/jm401958n
72737750 121301 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335543 121301 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 299 5 0 2 3.7 Fc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
137640152 163532 0 None -1995 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 631 15 3 10 4.0 CCCCn1cc(CCCOc2ccc(C(=O)NCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
CHEMBL4070604 163532 0 None -1995 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 631 15 3 10 4.0 CCCCn1cc(CCCOc2ccc(C(=O)NCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
155514430 176643 0 None -14 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 310 6 0 3 3.8 CCCCN1CCN(c2cc(CC)cc(Cl)c2OC)CC1 10.1021/acs.jmedchem.6b00860
CHEMBL4440301 176643 0 None -14 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 310 6 0 3 3.8 CCCCN1CCN(c2cc(CC)cc(Cl)c2OC)CC1 10.1021/acs.jmedchem.6b00860
168270455 196812 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5171772 196812 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
155195501 176872 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 410 7 2 6 3.2 C[C@H]1COC(c2ccc(N)nc2)CN1CCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.9b00702
CHEMBL4443441 176872 0 None -28 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 410 7 2 6 3.2 C[C@H]1COC(c2ccc(N)nc2)CN1CCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.9b00702
168270455 196812 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5171772 196812 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
168270455 196812 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5171772 196812 0 None 1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 406 5 1 2 5.8 Fc1cc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5280960 200869 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 336 5 0 5 3.2 Cc1cccc(COC2CCN(Cc3cn4ccccc4n3)CC2)n1 10.1016/j.ejmech.2022.114840
44355433 28951 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 383 8 0 3 5.9 CCCN(CCc1cccs1)C1CCc2c(cccc2OC2CCCC2)C1 10.1021/jm960345l
CHEMBL132261 28951 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 383 8 0 3 5.9 CCCN(CCc1cccs1)C1CCc2c(cccc2OC2CCCC2)C1 10.1021/jm960345l
10642702 45984 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 366 4 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL147003 45984 0 None -2 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 366 4 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
12997413 13900 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
CHEMBL108527 13900 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
44431494 155529 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2cccnc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL394042 155529 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 345 4 1 3 3.6 O=C(NC1CCN(Cc2cccnc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
154725389 183427 1 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 11 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)C(C)C 10.1021/acs.jmedchem.9b01835
CHEMBL4453405 183427 1 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 11 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)C(C)C 10.1021/acs.jmedchem.9b01835
CHEMBL4598003 183427 1 None -3 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 11 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)C(C)C 10.1021/acs.jmedchem.9b01835
3198 212292 76 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 212292 76 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 212292 76 None -26 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
122180569 128499 0 None -208 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.0 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588914 128499 0 None -208 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.0 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
44431459 94097 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccccc2Cl)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL233214 94097 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccccc2Cl)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
53248361 68856 0 None -213 7 Human 6.5 pKi = 6.5 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 568 7 0 5 3.2 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52I)c2ccccn2)CC1 10.1021/jm1009956
CHEMBL1774991 68856 0 None -213 7 Human 6.5 pKi = 6.5 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 568 7 0 5 3.2 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52I)c2ccccn2)CC1 10.1021/jm1009956
10782049 26798 0 None 10 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL130347 26798 0 None 10 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 321 9 1 3 4.5 Clc1ccc(SCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
155515759 176784 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 533 12 2 7 4.1 COc1ccc(N(Cc2cccc(OC)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4442419 176784 0 None 3 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 533 12 2 7 4.1 COc1ccc(N(Cc2cccc(OC)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
109030515 182764 1 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 182764 1 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
25070419 118555 0 None -9 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cc4ccccn4n3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287394 118555 0 None -9 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3cc4ccccn4n3)CC2)c1Cl 10.1021/jm5004039
44405414 78595 0 None 1148 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccccc2F)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL196866 78595 0 None 1148 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccccc2F)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
11678172 84807 0 None -72 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL209876 84807 0 None -72 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
118709160 120183 0 None -2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 846 18 0 8 10.1 O=C(CCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318832 120183 0 None -2 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 846 18 0 8 10.1 O=C(CCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709173 120198 0 None -19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 20 0 10 9.4 O=C(CCN1CCN(CCC(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318846 120198 0 None -19 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 944 20 0 10 9.4 O=C(CCN1CCN(CCC(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
22727324 20200 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 409 8 0 5 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3ccc(F)cc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1192902 20200 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 409 8 0 5 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3ccc(F)cc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL544220 20200 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 409 8 0 5 4.6 COc1ccccc1N1CCN(CCCCc2cc(-c3ccc(F)cc3)no2)CC1 10.1016/s0960-894x(02)00179-8
681 8247 72 None -2 38 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
940 8247 72 None -2 38 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
947 8247 72 None -2 38 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
CHEMBL59 8247 72 None -2 38 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
DB00988 8247 72 None -2 38 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
9975465 194430 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49502 194430 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
10086123 118261 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 299 1 0 1 4.9 C=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL327713 118261 0 None -9 3 Human 6.5 pKi = 6.5 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 299 1 0 1 4.9 C=C1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
72205045 98721 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 380 6 0 4 4.3 Clc1ccc(-n2cc(CCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414356 98721 0 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 380 6 0 4 4.3 Clc1ccc(-n2cc(CCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
44436606 98772 0 None -102 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241641 98772 0 None -102 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
102262219 146837 0 None -6918 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800400 146837 0 None -6918 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
15508238 11567 1 None 2 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 340 3 0 2 4.7 C(#Cc1cccn1C1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(99)00540-5
CHEMBL104092 11567 1 None 2 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 340 3 0 2 4.7 C(#Cc1cccn1C1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(99)00540-5
44319370 113824 0 None 1 4 Human 5.5 pKi = 5.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
CHEMBL315564 113824 0 None 1 4 Human 5.5 pKi = 5.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
134156222 161130 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
CHEMBL3986927 161130 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
44283889 126899 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 5 0 4 3.0 COc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL35114 126899 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 365 5 0 4 3.0 COc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1 10.1016/s0960-894x(98)00252-2
134156222 161130 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
CHEMBL3986927 161130 0 None -50 8 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 334 5 1 3 3.2 O=C1Cc2cc(C(=O)CCCN3CCc4ccccc4C3)ccc2N1 10.1016/j.bmc.2016.09.019
130431337 180866 0 None -2344 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4544583 180866 0 None -2344 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 438 8 2 3 4.7 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
44336052 12206 0 None 19 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 C[C@H]1CN(Cc2ccc(Cl)cc2)[C@H](C)CN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL107351 12206 0 None 19 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 C[C@H]1CN(Cc2ccc(Cl)cc2)[C@H](C)CN1CC(=O)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
10801405 33179 1 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
CHEMBL135944 33179 1 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)[C@H]1CCc2ccc(OC)cc2C1 10.1021/jm960345l
44393403 71852 0 None -125 6 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL182379 71852 0 None -125 6 Human 6.5 pKi = 6.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
53248213 68808 0 None -851 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
CHEMBL1774535 68808 0 None -851 5 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 7 2 3 4.8 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm200288r
164627741 193284 0 None -128 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4877460 193284 0 None -128 3 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 427 6 2 5 3.8 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
71062708 161085 0 None -19 12 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3986651 161085 0 None -19 12 Mouse 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
168294968 199198 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5208124 199198 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.bmcl.2022.128615
168294968 199198 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5208124 199198 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.ejmech.2022.114840
168294968 199198 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5208124 199198 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 0 4 3.8 Fc1ccc(COC2CCN(Cc3cn4ccccc4n3)CC2)cc1F 10.1016/j.ejmech.2022.114840
10276451 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm0611152
CHEMBL2112910 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm0611152
CHEMBL59725 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm0611152
CHEMBL5092747 222164 0 None -16 5 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL None None None CC(=O)Nc1ccc(-c2cc(-c3ccccc3)nc3cc(C(=O)NCCCn4ccnc4)nn23)cc1 10.6019/CHEMBL5058647
CHEMBL5092747 222164 0 None -16 5 Human 5.5 pKi = 5.5 Binding
GPCRScan assay: inhibition of D4GPCRScan assay: inhibition of D4
ChEMBL None None None CC(=O)Nc1ccc(-c2cc(-c3ccccc3)nc3cc(C(=O)NCCCn4ccnc4)nn23)cc1 10.6019/CHEMBL5058647
25895957 11616 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 414 5 0 5 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2cc([N+](=O)[O-])ccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104251 11616 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 414 5 0 5 3.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2cc([N+](=O)[O-])ccc21 10.1016/s0960-894x(02)00655-8
10641954 213710 0 None 77 2 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1Cl)CC3 10.1021/jm970170v
CHEMBL91067 213710 0 None 77 2 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1Cl)CC3 10.1021/jm970170v
10335148 85661 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 303 4 1 2 3.9 C1=C(c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
CHEMBL2112912 85661 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 303 4 1 2 3.9 C1=C(c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
21465540 118192 1 None - 1 Human 7.5 pKi = 7.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 337 4 2 3 2.8 O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL327310 118192 1 None - 1 Human 7.5 pKi = 7.5 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 337 4 2 3 2.8 O=C(NC(=O)c1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
2946349 106509 7 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 325 7 1 3 3.4 OC(COc1ccccc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL284892 106509 7 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 325 7 1 3 3.4 OC(COc1ccccc1)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
9975465 194430 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
CHEMBL49502 194430 0 None 109 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1021/jm970021c
10641954 213710 0 None 77 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1Cl)CC3 10.1016/j.ejmech.2020.113034
CHEMBL91067 213710 0 None 77 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccccc1Cl)CC3 10.1016/j.ejmech.2020.113034
44403210 77318 0 None -7 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 385 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL194727 77318 0 None -7 5 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 385 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
10137748 59835 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1cc(C)ccc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
CHEMBL159742 59835 0 None 28 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1cc(C)ccc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
71652196 94229 0 None 15 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 368 4 1 5 3.6 Oc1ccc(N2CCN(Cc3cnn(-c4ccc(Cl)cc4)c3)CC2)cc1 10.1016/j.ejmech.2012.08.011
CHEMBL2333732 94229 0 None 15 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 368 4 1 5 3.6 Oc1ccc(N2CCN(Cc3cnn(-c4ccc(Cl)cc4)c3)CC2)cc1 10.1016/j.ejmech.2012.08.011
191 7191 98 None -8 29 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
201 7191 98 None -8 29 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
2170 7191 98 None -8 29 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
CHEMBL1113 7191 98 None -8 29 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
DB00543 7191 98 None -8 29 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1021/jm2013419
44431481 94810 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL234472 94810 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
137643951 165038 0 None -23 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4088639 165038 0 None -23 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
16105549 74560 0 None -75 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
CHEMBL1908879 74560 0 None -75 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
CHEMBL221640 74560 0 None -75 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
122181330 128649 0 None -39 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590081 128649 0 None -39 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
56833378 75108 0 None -18 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916549 75108 0 None -18 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
44276050 20052 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 9 0 5 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1191675 20052 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 9 0 5 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL542809 20052 0 None -3 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 9 0 5 4.9 CCOc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
22727331 20099 0 None -5 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1192096 20099 0 None -5 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL543278 20099 0 None -5 3 Human 7.5 pKi = 7.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 451 10 0 7 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4OC)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
44438228 100331 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246438 100331 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
19958494 106229 1 None 9 4 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL283036 106229 1 None 9 4 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 360 3 1 3 3.9 FC(F)(F)c1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
127052467 147629 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819494 147629 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
10276451 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049612a
CHEMBL2112910 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049612a
CHEMBL59725 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm049612a
10276451 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
CHEMBL2112910 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
CHEMBL59725 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
10276451 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
CHEMBL2112910 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
CHEMBL59725 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
10276451 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL2112910 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL59725 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
44381117 64605 0 None 25 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL167032 64605 0 None 25 4 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
72545010 99900 0 None 7 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443003 99900 0 None 7 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
44319102 212920 0 None 2 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL86060 212920 0 None 2 4 Human 6.5 pKi = 6.5 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
10276451 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL2112910 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL59725 207064 37 None -776 9 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
45483654 204897 0 None -14 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7cccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)c7)nn6)cc5)cc4)nn3)c2)CC1 10.1021/jm901120h
CHEMBL574569 204897 0 None -14 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7cccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)c7)nn6)cc5)cc4)nn3)c2)CC1 10.1021/jm901120h
135545150 45246 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 3 2 5 3.6 Clc1ccc2c(c1)C(NCCN1CCCC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL146410 45246 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 3 2 5 3.6 Clc1ccc2c(c1)C(NCCN1CCCC1)=Nc1cccnc1N2 10.1021/jm0104825
71658076 97177 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccccc3)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386615 97177 0 None -38 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 463 9 1 5 5.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccccc3)s2)CC1 10.1016/j.bmc.2013.03.074
60165539 82127 0 None 5 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 5 4.7 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037524 82127 0 None 5 3 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 399 6 0 5 4.7 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL5075990 221186 0 None -31 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NCC2CCCN2CCCCNCCC(C(=O)N(C)C)(c2ccccc2)c2ccccc2)c1O 10.1021/acs.jmedchem.1c00611
168291477 198660 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5199649 198660 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.ejmech.2022.114840
168291477 198660 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5199649 198660 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.bmcl.2022.128615
42626318 63010 0 None -3090 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627306 63010 0 None -3090 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
49799693 21167 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccc(OCCF)cc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1173366 21167 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccc(OCCF)cc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200278 21167 0 None -25 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccc(OCCF)cc23)CC1 10.1016/j.bmc.2010.05.052
11144835 126471 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 449 9 1 4 4.7 COc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL347290 126471 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 449 9 1 4 4.7 COc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
127051843 147529 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 147529 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44395714 19637 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 385 6 0 2 5.9 O=C(CCCN1C2CCC1CC(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL1188714 19637 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 385 6 0 2 5.9 O=C(CCCN1C2CCC1CC(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL537182 19637 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 385 6 0 2 5.9 O=C(CCCN1C2CCC1CC(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
11849181 86835 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
CHEMBL213004 86835 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.5 CO/N=C(/c1ccc(Cl)cc1)C(C)CN1CCN(c2ccccn2)CC1 10.1021/jm060279f
60165411 82132 0 None -95 5 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 381 7 0 7 3.3 O=C(CCCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037529 82132 0 None -95 5 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 381 7 0 7 3.3 O=C(CCCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
22727356 20098 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 387 8 0 4 5.0 C(=C/c1cc(CCCCN2CCN(c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL1192095 20098 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 387 8 0 4 5.0 C(=C/c1cc(CCCCN2CCN(c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL543277 20098 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 387 8 0 4 5.0 C(=C/c1cc(CCCCN2CCN(c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
168291477 198660 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5199649 198660 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 343 6 0 3 4.3 COc1ccc(CN2CCC[C@H](OCc3ccccc3C)C2)cc1F 10.1016/j.ejmech.2022.114840
127051843 147529 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818200 147529 0 None -15 9 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 0 3 3.6 N#Cc1ccc(C(=O)CCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
44438220 100225 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 381 4 2 2 4.4 CC(=O)NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246021 100225 0 None -4 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 381 4 2 2 4.4 CC(=O)NC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
12066265 103886 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 487 6 0 2 7.6 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccc(Cl)c(Cl)c2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL267562 103886 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 487 6 0 2 7.6 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccc(Cl)c(Cl)c2)c2ccc(F)cc2)cc1 10.1021/jm010146o
44339953 116477 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
CHEMBL322802 116477 0 None 3 4 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
10436653 39566 1 None -51 5 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 521 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[te]2)CC1 10.1021/jm025558r
CHEMBL141419 39566 1 None -51 5 Human 7.5 pKi = 7.5 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 521 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[te]2)CC1 10.1021/jm025558r
127031500 146128 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792931 146128 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 323 5 0 5 2.6 c1ccc(OC[C@@H]2CN(Cc3ncn4ccccc34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
71460561 88597 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 435 6 0 5 4.5 O=C(c1cnc2ccccc2n1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164346 88597 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 435 6 0 5 4.5 O=C(c1cnc2ccccc2n1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
127052467 147629 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
CHEMBL3819494 147629 0 None 1 7 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 304 5 1 1 4.5 c1ccc2c(c1)CCN(CCCCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2016.05.053
57391306 76934 0 None 6 5 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 0 2 4.9 [O-][S+](CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940407 76934 0 None 6 5 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 379 6 0 2 4.9 [O-][S+](CCCN1CCC(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
90644227 118557 0 None -26 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287396 118557 0 None -26 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
44436617 98335 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 481 9 1 4 4.8 COc1ccccc1N1CCN(CCCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL240584 98335 0 None -1 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 481 9 1 4 4.8 COc1ccccc1N1CCN(CCCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
11176211 11563 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 372 8 0 6 3.3 CCOc1ccccc1OCC1CN(Cc2ccc([N+](=O)[O-])cc2)CCO1 10.1021/jm031111m
CHEMBL104079 11563 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 372 8 0 6 3.3 CCOc1ccccc1OCC1CN(Cc2ccc([N+](=O)[O-])cc2)CCO1 10.1021/jm031111m
44283891 126968 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 363 4 0 3 3.6 Cc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL35182 126968 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 363 4 0 3 3.6 Cc1ccc(N2CCN(CCC3c4ccccc4C(=O)N3C)CC2)cc1C 10.1016/s0960-894x(98)00252-2
90644059 118807 0 None 22 3 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289643 118807 0 None 22 3 Rat 7.5 pKi = 7.5 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
10714184 85377 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 369 5 1 3 5.1 CC1(C(=O)/C=C(\O)c2ccc(Cl)cc2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
CHEMBL2112284 85377 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 369 5 1 3 5.1 CC1(C(=O)/C=C(\O)c2ccc(Cl)cc2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
10972865 210507 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
CHEMBL67750 210507 0 None -3 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 479 6 1 3 5.5 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
71657947 97172 0 None -93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 415 8 1 4 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386610 97172 0 None -93 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 415 8 1 4 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2013.03.074
145986441 173951 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 432 7 2 4 3.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Br)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4291172 173951 0 None -102 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 432 7 2 4 3.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Br)cc1)CC2 10.1021/acsmedchemlett.8b00229
12050198 207033 0 None 17 4 Human 6.5 pKi = 6.5 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 347 6 1 4 4.1 c1ccc(CN2CCC(NCc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59702 207033 0 None 17 4 Human 6.5 pKi = 6.5 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 347 6 1 4 4.1 c1ccc(CN2CCC(NCc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
92716 79108 22 None 5 2 Human 6.5 pKi = 6.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 301 2 4 5 2.3 CN1CCc2cc(O)c(O)cc2C1Cc1ccc(O)c(O)c1 10.1016/S0960-894X(97)00194-7
CHEMBL19844 79108 22 None 5 2 Human 6.5 pKi = 6.5 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 301 2 4 5 2.3 CN1CCc2cc(O)c(O)cc2C1Cc1ccc(O)c(O)c1 10.1016/S0960-894X(97)00194-7
44381286 127145 0 None -1 4 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL353220 127145 0 None -1 4 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
380039 21080 5 None -5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 391 3 0 4 4.2 CN1CN(c2ccccc2)C2(CCN(Cc3csc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1169728 21080 5 None -5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 391 3 0 4 4.2 CN1CN(c2ccccc2)C2(CCN(Cc3csc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1199909 21080 5 None -5 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 391 3 0 4 4.2 CN1CN(c2ccccc2)C2(CCN(Cc3csc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
44438224 161415 0 None -60 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 396 5 1 3 4.9 CCOC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL399396 161415 0 None -60 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 396 5 1 3 4.9 CCOC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
122180570 128500 0 None -114 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 3.9 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588915 128500 0 None -114 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 430 8 1 6 3.9 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc4[nH]ccc4c3)nn2)CC1 10.1016/j.bmc.2015.01.017
44438199 158098 3 None -27 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2cccc(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL396092 158098 3 None -27 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 340 3 2 2 4.3 OC1(c2cccc(Cl)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL5091479 222089 1 None -4 2 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN1CCC(c2ccccc2)(c2ccccc2)C1 10.1021/acs.jmedchem.1c00611
44330585 215087 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 2 0 3 4.8 CCCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL99085 215087 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 300 2 0 3 4.8 CCCn1ncc2c1-c1c(Cl)sc(Cl)c1CCC2 10.1016/s0960-894x(03)00587-0
130431325 179191 0 None -2290 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 4 5.0 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4476699 179191 0 None -2290 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 4 5.0 CCc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
11809415 127741 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 0 1 5 3.2 Cc1ccc2c(c1)C(N1CCCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL356171 127741 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 0 1 5 3.2 Cc1ccc2c(c1)C(N1CCCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
11784937 128653 19 None -11220 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm501512b
CHEMBL3590085 128653 19 None -11220 3 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 481 7 0 7 4.7 Cc1ncoc1-c1nnc(SCCCN2C[C@@H]3C[C@]3(c3ccc(C(F)(F)F)cc3F)C2)n1C 10.1021/jm501512b
155195496 177495 0 None -72 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4452064 177495 0 None -72 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
ChEMBL 407 7 3 5 3.1 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CCCCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
10063875 109098 0 None -389 5 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 308 4 2 3 2.7 O=C1Cc2c(ccc3c2O[C@@H](CNCc2ccccc2)CC3)N1 10.1016/s0960-894x(01)00778-8
CHEMBL303556 109098 0 None -389 5 Human 6.5 pKi = 6.5 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 308 4 2 3 2.7 O=C1Cc2c(ccc3c2O[C@@H](CNCc2ccccc2)CC3)N1 10.1016/s0960-894x(01)00778-8
56675269 73184 2 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1016/j.bmc.2011.04.021
CHEMBL1813585 73184 2 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1016/j.bmc.2011.04.021
CHEMBL1851858 73184 2 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 409 8 1 5 3.6 COc1ccc(N2CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)cc1 10.1016/j.bmc.2011.04.021
44394599 73008 0 None 85 2 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccccc1-c1ccc(C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL184551 73008 0 None 85 2 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccccc1-c1ccc(C(=O)NC2CCN(Cc3ccccc3)C2)cc1 10.1016/j.bmcl.2004.07.045
135398737 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
38 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
722 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
CHEMBL42 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
DB00363 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
44436301 97407 0 None 4 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 433 6 0 5 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238915 97407 0 None 4 4 Human 7.4 pKi = 7.4 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 433 6 0 5 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2021.128028
10472143 126055 0 None -81 16 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 126055 0 None -81 16 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
9867004 176047 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCC2 10.1016/s0960-894x(02)00655-8
CHEMBL441274 176047 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2CC12CCCC2 10.1016/s0960-894x(02)00655-8
155529568 178232 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 385 6 1 5 3.5 COc1ccccc1N1CCN(CCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4463276 178232 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 385 6 1 5 3.5 COc1ccccc1N1CCN(CCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
155554837 181415 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4558031 181415 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
127031201 146153 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3793131 146153 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 372 6 0 5 3.5 COc1ccc(CN2CCO[C@H](COc3cccc(C#N)c3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
127031513 146252 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
CHEMBL3794287 146252 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1cccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)c1 10.1016/j.bmcl.2016.03.102
90644059 118807 0 None 22 3 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289643 118807 0 None 22 3 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
16725931 157819 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL395867 157819 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
122181327 128646 0 None -50 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 431 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590078 128646 0 None -50 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 431 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
3802 209802 21 None -1 5 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL63329 209802 21 None -1 5 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
72737723 9356 1 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
8440 9356 1 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
CHEMBL3335556 9356 1 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 10.1021/ml500267c
155554837 181415 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
CHEMBL4558031 181415 0 None -2 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 4 0 4 3.8 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cn2)CC1 10.1016/j.bmc.2020.115943
76318473 113071 0 None -95 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 510 13 2 6 3.7 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3cc(OCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133868 113071 0 None -95 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 510 13 2 6 3.7 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3cc(OCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139054 113071 0 None -95 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 510 13 2 6 3.7 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3cc(OCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
57393627 76082 0 None -40 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928131 76082 0 None -40 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
118709162 120185 0 None -125 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 874 20 0 8 10.9 O=C(CCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318834 120185 0 None -125 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 874 20 0 8 10.9 O=C(CCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
45270861 201859 0 None 11 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 353 3 0 5 3.1 Cc1cc2nc(C)c(CN3CCN(c4ccc(F)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL549638 201859 0 None 11 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 353 3 0 5 3.1 Cc1cc2nc(C)c(CN3CCN(c4ccc(F)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
11078813 118795 0 None 6 4 Human 5.4 pKi = 5.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 356 4 1 5 2.8 OCc1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
CHEMBL328925 118795 0 None 6 4 Human 5.4 pKi = 5.4 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 356 4 1 5 2.8 OCc1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
10973768 114337 0 None -9332 10 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL318901 114337 0 None -9332 10 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
10276451 207064 37 None -776 9 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL2112910 207064 37 None -776 9 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
CHEMBL59725 207064 37 None -776 9 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in CHO cells
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm040190e
71086303 167589 0 None -1 2 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL4114493 167589 0 None -1 2 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
168293874 198958 0 None -83 11 Human 6.4 pKi = 6.4 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 198958 0 None -83 11 Human 6.4 pKi = 6.4 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
44426502 148844 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL387952 148844 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 386 7 1 2 5.1 O=C(NC1CCN(CCCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
44309688 210771 0 None -15 4 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2 10.1021/jm040190e
CHEMBL69571 210771 0 None -15 4 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2 10.1021/jm040190e
25132869 110072 0 None -57 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
CHEMBL3084503 110072 0 None -57 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptorDisplacement of [125I]IABN from human dopamine D4 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
44438221 155558 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 342 3 1 1 5.3 FC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL394065 155558 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 342 3 1 1 5.3 FC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
122181007 128574 0 None -15848 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 509 7 2 4 4.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)-c1ccccc1C2 10.1016/j.bmc.2015.01.017
CHEMBL3589652 128574 0 None -15848 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 509 7 2 4 4.9 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)-c1ccccc1C2 10.1016/j.bmc.2015.01.017
6674 9593 26 None -2691 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
9891901 9593 26 None -2691 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
CHEMBL300780 9593 26 None -2691 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 493 7 1 3 5.9 O=C(c1ccc2c(c1)Cc1c2cccc1)NCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
11812065 210799 7 None -91 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 431 6 0 4 4.2 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
CHEMBL69717 210799 7 None -91 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 431 6 0 4 4.2 O=C1c2ccccc2C(=O)N1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm010146o
CHEMBL5077645 221288 0 None -97723 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None Oc1cccc([C@@]23CCC[C@@H]([C@H]2O)N(C/C=C/c2ccccc2)CC3)c1 10.1021/acs.jmedchem.1c00611
10403435 20222 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 315 3 0 2 5.2 C=CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1193072 20222 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 315 3 0 2 5.2 C=CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL544418 20222 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 315 3 0 2 5.2 C=CCN1CC=C(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
9820313 112971 0 None -1 4 Human 7.4 pKi = 7.4 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 361 4 2 3 4.1 FC(F)(F)c1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL313851 112971 0 None -1 4 Human 7.4 pKi = 7.4 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 361 4 2 3 4.1 FC(F)(F)c1nc2c3c(ccc2[nH]1)CCC(CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
44335896 12148 0 None 45 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106998 12148 0 None 45 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44336005 12215 0 None 60 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 3 4.0 CC1CCc2cc(F)ccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107391 12215 0 None 60 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 3 4.0 CC1CCc2cc(F)ccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
57399494 77232 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
CHEMBL1946124 77232 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
155564110 182148 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4574793 182148 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
57399494 77232 0 None -1 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2012.01.022
CHEMBL1946124 77232 0 None -1 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2012.01.022
134146195 161370 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3941795 161370 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3991399 161370 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
127032084 146119 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792813 146119 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 322 5 1 3 3.4 c1ccc(OC[C@@H]2CN(Cc3cccc4cc[nH]c34)CCO2)cc1 10.1016/j.bmcl.2016.03.102
127031830 146210 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793906 146210 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 356 5 1 3 4.1 Clc1ccc2[nH]cc(CN3CCO[C@H](COc4ccccc4)C3)c2c1 10.1016/j.bmcl.2016.03.102
10385977 104106 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL26929 104106 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 394 7 0 4 4.7 COc1ccccc1N1CCN(CCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
44431479 94355 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL233581 94355 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
122189387 130020 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 417 7 0 8 2.7 COc1ccccc1N1CCN(CCCc2cn(-c3ccn4nccc4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613873 130020 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 417 7 0 8 2.7 COc1ccccc1N1CCN(CCCc2cn(-c3ccn4nccc4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
71734028 97828 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
CHEMBL2397390 97828 0 None -11 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
11079832 171692 0 None 16 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 1 5 4.4 Cc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL422310 171692 0 None 16 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 1 5 4.4 Cc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
44372153 126942 0 None 83 4 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 416 4 0 4 5.3 Cc1nn2c(-c3ccccc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL351550 126942 0 None 83 4 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 416 4 0 4 5.3 Cc1nn2c(-c3ccccc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
57399494 77232 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
CHEMBL1946124 77232 0 None 1 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 386 4 0 3 4.4 O=C1c2ccc(F)cc2CC1CCN1CCCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2020.115943
155564110 182148 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4574793 182148 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 375 6 0 4 4.0 O=C(CCCN1CCCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
134146195 161370 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3941795 161370 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3991399 161370 0 None -3 9 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 362 5 0 3 5.8 Clc1ccc2sc(CCCCN3CCC4CCCCC4C3)nc2c1 10.1016/j.bmc.2016.09.019
139877715 199601 0 None 21 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 321 5 0 4 3.6 c1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5179879 199601 0 None 21 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 321 5 0 4 3.6 c1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221531 199601 0 None 21 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 321 5 0 4 3.6 c1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1021/acs.jmedchem.2c00840
9906454 145049 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 5 1 4 2.7 COc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL37706 145049 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 351 5 1 4 2.7 COc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1 10.1016/s0960-894x(98)00252-2
10939408 54197 0 None -125 5 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm020952a
CHEMBL154508 54197 0 None -125 5 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 455 7 1 3 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2ccccc2c1 10.1021/jm020952a
12050197 107651 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 6 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL293645 107651 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 457 6 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
12049521 209970 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 427 5 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64288 209970 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 427 5 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
44381276 65502 0 None 2 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL168541 65502 0 None 2 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
3228 9920 23 None -4168 7 Human 5.4 pKi = 5.4 Binding
Displacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay basedDisplacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
9909448 9920 23 None -4168 7 Human 5.4 pKi = 5.4 Binding
Displacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay basedDisplacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
CHEMBL71838 9920 23 None -4168 7 Human 5.4 pKi = 5.4 Binding
Displacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay basedDisplacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
10086348 14824 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1021/jm950721m
CHEMBL109101 14824 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1021/jm950721m
10086348 14824 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1016/j.bmcl.2005.02.012
CHEMBL109101 14824 0 None -144 4 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 303 3 1 3 3.2 Nc1ccc(C#CCCN2CC=C(c3ccccc3)CC2)nc1 10.1016/j.bmcl.2005.02.012
164619127 192304 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 192304 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
71657943 97168 0 None -128 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 9 1 5 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(SC)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386606 97168 0 None -128 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 9 1 5 4.1 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(SC)cc2)CC1 10.1016/j.bmc.2013.03.074
10254390 78463 0 None -2884 7 Rat 6.4 pKi = 6.4 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm050171k
CHEMBL196476 78463 0 None -2884 7 Rat 6.4 pKi = 6.4 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm050171k
164619127 192304 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
CHEMBL4862770 192304 0 None -32 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 428 10 2 4 4.8 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCCOc1ccc2c(c1)NC(=O)CC2 10.1021/acs.jmedchem.1c01327
168277394 197180 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5177641 197180 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)cc1F 10.1016/j.bmcl.2022.128615
6917970 10463 61 None -851 33 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
8370 10463 61 None -851 33 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
CHEMBL487387 10463 61 None -851 33 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
11477180 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm049465g
6675 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm049465g
CHEMBL180010 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm049465g
11778580 72901 1 None -645 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
CHEMBL184050 72901 1 None -645 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
11477180 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm200288r
6675 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm200288r
CHEMBL180010 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm200288r
11477180 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
6675 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
CHEMBL180010 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0704200
11477180 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
6675 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
CHEMBL180010 9848 6 None -616 6 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cellsInhibition of [125I]IABN binding to human Dopamine D4 receptor expressed in HEK 293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm040190e
44438203 100430 2 None -34 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 4.7 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246848 100430 2 None -34 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 374 3 2 2 4.7 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
17756213 156483 1 None -58 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
CHEMBL394779 156483 1 None -58 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
11300847 211769 1 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1cncc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
CHEMBL76653 211769 1 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 293 3 1 4 2.3 c1cncc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
154706431 183364 1 None -33 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4531363 183364 1 None -33 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597531 183364 1 None -33 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
49798833 21132 0 None -8 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 323 3 1 3 4.4 OC1(c2ccccc2)CCN(Cc2cc3ccccc3s2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172212 21132 0 None -8 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 323 3 1 3 4.4 OC1(c2ccccc2)CCN(Cc2cc3ccccc3s2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200152 21132 0 None -8 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 323 3 1 3 4.4 OC1(c2ccccc2)CCN(Cc2cc3ccccc3s2)CC1 10.1016/j.bmc.2010.05.052
CHEMBL5073754 221084 0 None -15 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
11716449 147993 0 None -20 4 Human 6.4 pKi = 6.4 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 147993 0 None -20 4 Human 6.4 pKi = 6.4 Binding
Inhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D4 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
4420454 63033 6 None 1 5 Human 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 63033 6 None 1 5 Human 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
10548105 25642 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
CHEMBL128222 25642 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1021/jm970422s
11256262 86776 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL212782 86776 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 7 0 5 3.0 CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
56837636 76072 0 None -26 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928121 76072 0 None -26 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
127046952 146879 0 None -3 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800636 146879 0 None -3 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
10548105 25642 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128222 25642 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 383 9 1 3 4.5 Clc1ccc(OCCNCCCOc2ccc(Br)cc2)cc1 10.1016/j.bmcl.2005.02.012
11199162 86634 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212235 86634 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 358 6 0 5 3.3 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
12899499 73397 0 None -7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 395 7 1 5 3.2 COc1ccccc1N1CCN(CCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813596 73397 0 None -7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 395 7 1 5 3.2 COc1ccccc1N1CCN(CCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1852734 73397 0 None -7 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 395 7 1 5 3.2 COc1ccccc1N1CCN(CCCOc2ccc3c(c2)NC(=O)CC3)CC1 10.1016/j.bmc.2011.04.021
CHEMBL5083473 221644 0 None 5 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(c3cccc(O)c3)c3cccc(OC)c3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
3038495 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0611152
7625 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0611152
CHEMBL25236 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0611152
4420454 63033 6 None 1 5 Human 6.4 pKi = 6.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 63033 6 None 1 5 Human 6.4 pKi = 6.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
11615489 76218 1 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL193337 76218 1 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm101639t
10039198 63123 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 63123 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL5072449 221060 0 None -8 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None O=C(NCCCCN1CC[C@]2(c3cccc(O)c3)CCC[C@H]1[C@H]2O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
90389592 154452 2 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL3931765 154452 2 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
90389592 154452 2 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
CHEMBL3931765 154452 2 None -12 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 422 8 1 4 2.8 CC(O)CN1CCN(CC[S+]([O-])C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
154705520 183039 1 None -25 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4452683 183039 1 None -25 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594959 183039 1 None -25 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
71455083 88605 0 None -239 7 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164354 88605 0 None -239 7 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
53325242 63844 0 None -1 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 63844 0 None -1 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
9907381 11669 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104514 11669 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 4 0 3 3.0 O=C(CN1CCc2ccccc21)N1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
72191064 99134 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 469 8 0 6 4.3 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(Br)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430442 99134 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 469 8 0 6 4.3 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(Br)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
44438211 154240 2 None -19 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.7 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL393027 154240 2 None -19 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 2 2 4.7 OC1(c2ccc(Cl)cc2)CCCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
54477 91428 36 None -14 22 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm00025a013
CHEMBL22242 91428 36 None -14 22 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC 10.1021/jm00025a013
3038495 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
7625 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
CHEMBL25236 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
135398737 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
38 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
722 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
CHEMBL42 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
DB00363 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
2865 10915 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
59 10915 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
60854 10915 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
CHEMBL708 10915 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
DB00246 10915 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
103 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
2875 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
5736 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
CHEMBL285802 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
DB09225 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
2865 10915 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
59 10915 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
60854 10915 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
CHEMBL708 10915 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
DB00246 10915 73 None -66 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
103 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
2875 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
5736 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
CHEMBL285802 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
DB09225 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
135398737 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
38 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
722 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
CHEMBL42 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
DB00363 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
57394810 76932 0 None 2 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 0 2 5.8 Fc1ccc(SCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940405 76932 0 None 2 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 0 2 5.8 Fc1ccc(SCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
49782601 24260 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 487 6 1 3 6.2 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1257810 24260 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 487 6 1 3 6.2 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
45267409 202940 0 None 676 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)ncn23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL561262 202940 0 None 676 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)ncn23)CC1 10.1016/j.bmc.2009.05.015
9906895 126734 2 None 25 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL349699 126734 2 None 25 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 360 4 0 5 2.7 Fc1ccc(OC[C@@H]2CC[C@@H]3CN(c4ncc(F)cn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
12050202 210077 0 None 43 4 Human 7.4 pKi = 7.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CN[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64752 210077 0 None 43 4 Human 7.4 pKi = 7.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CN[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
45379369 14294 0 None -15 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
CHEMBL1087300 14294 0 None -15 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]radioligand from human recombinant dopamine D4.4 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
8592415 71943 6 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL182432 71943 6 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
10477871 90005 0 None -158 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc(C#N)cc3[nH]2)CC1 10.1021/jm0611152
CHEMBL218638 90005 0 None -158 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 431 8 2 5 3.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc(C#N)cc3[nH]2)CC1 10.1021/jm0611152
11570589 91024 0 None -18 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 582 13 1 7 4.8 CCCc1c(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
CHEMBL221129 91024 0 None -18 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 582 13 1 7 4.8 CCCc1c(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
135398737 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
38 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
722 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
CHEMBL42 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
DB00363 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm070516u
4064342 213820 31 None -4 3 Human 6.4 pKi = 6.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 309 4 2 2 3.5 O=C(Nc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91621 213820 31 None -4 3 Human 6.4 pKi = 6.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 309 4 2 2 3.5 O=C(Nc1ccccc1)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
12050199 107589 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 7 1 5 4.9 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL293225 107589 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 455 7 1 5 4.9 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
44304652 207101 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59749 207101 0 None 1 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
44319368 112841 0 None -1 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
CHEMBL313320 112841 0 None -1 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
10824155 64014 1 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 243 5 0 1 3.6 C#CC(C#C)=C1CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL165022 64014 1 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4
ChEMBL 243 5 0 1 3.6 C#CC(C#C)=C1CCC(N(CCC)CCC)CC1 10.1021/jm991098z
164622629 192375 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Cl)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4863748 192375 0 None -20 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Cl)CC2 10.1016/j.bmcl.2021.128047
10885524 109903 0 None -38 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 7 1 3 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
CHEMBL307800 109903 0 None -38 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 7 1 3 5.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)C1c2ccccc2-c2ccccc21 10.1021/jm010146o
10572985 170261 0 None 1 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1ccc2c(c1)C(CCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
CHEMBL420067 170261 0 None 1 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1ccc2c(c1)C(CCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
1016 10519 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 10519 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 10519 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 10519 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 10519 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 10519 78 None -28 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
71061611 155839 0 None -10 3 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 356 6 0 4 3.0 Fc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3942898 155839 0 None -10 3 Mouse 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 356 6 0 4 3.0 Fc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
155522719 177569 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 298 4 1 6 0.6 O=C(CN1CCN(c2ccccn2)CC1)Nc1cncnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4453069 177569 0 None - 1 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 298 4 1 6 0.6 O=C(CN1CCN(c2ccccn2)CC1)Nc1cncnc1 10.1021/acs.jmedchem.9b00231
135404757 127736 0 None 2 2 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 1 2 5 3.6 CN1CCC(NC2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
CHEMBL356149 127736 0 None 2 2 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 341 1 2 5 3.6 CN1CCC(NC2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm0104825
44438213 100184 5 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.4 OC1(Cc2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL245815 100184 5 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 4 2 2 4.4 OC1(Cc2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
44438223 100267 0 None -64 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 1 3 4.5 COC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246231 100267 0 None -64 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 4 1 3 4.5 COC(=O)C1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL5077104 221260 0 None -64 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCCCC(=O)N1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
70788951 33928 1 None -1 5 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
CHEMBL1366 33928 1 None -1 5 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL None None None None nan
72191065 99133 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 421 9 0 7 3.6 COc1ccc(-c2cn(CCCCN3CCN(c4ccccc4OC)CC3)nn2)cc1 10.1016/j.bmcl.2013.08.047
CHEMBL2430441 99133 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 421 9 0 7 3.6 COc1ccc(-c2cn(CCCCN3CCN(c4ccccc4OC)CC3)nn2)cc1 10.1016/j.bmcl.2013.08.047
118719798 122503 0 None -309 4 Human 6.4 pKi = 6.4 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 473 9 0 7 5.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353901 122503 0 None -309 4 Human 6.4 pKi = 6.4 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 473 9 0 7 5.1 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
44356253 18350 0 None -794 5 Human 6.4 pKi = 6.4 Binding
Compound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, scCompound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, sc
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)OC(CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL1180604 18350 0 None -794 5 Human 6.4 pKi = 6.4 Binding
Compound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, scCompound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, sc
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)OC(CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL134808 18350 0 None -794 5 Human 6.4 pKi = 6.4 Binding
Compound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, scCompound was tested to inhibit Dopa accumulation in Dopamine receptor D4 at 10 mg/kg, sc
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)OC(CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
46231784 208117 0 None -6606 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604314 208117 0 None -6606 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
11762743 110591 0 None -109 4 Human 5.4 pKi = 5.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 6 1 4 5.1 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL309118 110591 0 None -109 4 Human 5.4 pKi = 5.4 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 493 6 1 4 5.1 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
44394884 129437 0 None 38 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.07.045
CHEMBL360394 129437 0 None 38 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 356 5 1 2 4.4 O=C(NC1CCN(Cc2ccccc2)C1)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.07.045
9951233 109567 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL305276 109567 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
10045525 210560 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL68191 210560 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(00)00421-2
44264682 104093 0 None 141 4 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)c1 10.1016/s0960-894x(98)00692-1
CHEMBL269202 104093 0 None 141 4 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 326 3 0 4 3.3 Clc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)c1 10.1016/s0960-894x(98)00692-1
11724450 130626 4 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to D34 (unknown origin) assessed as inhibition constantBinding affinity to D34 (unknown origin) assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL184158 130626 4 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to D34 (unknown origin) assessed as inhibition constantBinding affinity to D34 (unknown origin) assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
CHEMBL362542 130626 4 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to D34 (unknown origin) assessed as inhibition constantBinding affinity to D34 (unknown origin) assessed as inhibition constant
ChEMBL 334 4 1 4 2.6 Cc1cccc(NC(=O)CN2CCN(c3ccccc3C#N)CC2)c1 10.1016/j.ejmech.2020.113141
9951233 109567 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/j.ejmech.2020.113141
CHEMBL305276 109567 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/j.ejmech.2020.113141
9799781 126982 0 None 52 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 375 3 0 3 3.0 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(CC5)C3=O)CC2)cc1 10.1016/j.ejmech.2020.113141
CHEMBL351963 126982 0 None 52 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 375 3 0 3 3.0 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(CC5)C3=O)CC2)cc1 10.1016/j.ejmech.2020.113141
10430183 212407 0 None -39 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
CHEMBL81728 212407 0 None -39 7 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 385 5 1 5 2.1 O=C(NCCN1CCN(c2cccc3c2OCCO3)CC1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00633
44335995 115241 0 None 54 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 397 5 0 3 3.8 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL319923 115241 0 None 54 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 397 5 0 3 3.8 CC[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
44336000 115765 0 None 288 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL321201 115765 0 None 288 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccccc2Cl)CC1 10.1016/s0960-894x(02)00656-x
44336050 12086 0 None 77 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 376 4 0 2 4.9 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1C 10.1016/s0960-894x(02)00655-8
CHEMBL106742 12086 0 None 77 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 376 4 0 2 4.9 Cc1ccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)cc1C 10.1016/s0960-894x(02)00655-8
9800164 11724 0 None 22 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104788 11724 0 None 22 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335796 11737 0 None 15 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104832 11737 0 None 15 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.9 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00655-8
9799781 126982 0 None 52 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 375 3 0 3 3.0 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(CC5)C3=O)CC2)cc1 10.1016/s0960-894x(02)01056-9
CHEMBL351963 126982 0 None 52 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 375 3 0 3 3.0 Cc1ccc(CN2CCN(C3CCc4cccc5c4N(CC5)C3=O)CC2)cc1 10.1016/s0960-894x(02)01056-9
10045525 210560 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(02)01056-9
CHEMBL68191 210560 0 None 5 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 383 4 0 3 3.4 CCN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1016/s0960-894x(02)01056-9
10543298 46629 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 314 4 0 2 4.8 C1=C(c2ccccc2)CCN(Cc2ccn(-c3ccccc3)c2)C1 10.1021/jm00025a013
CHEMBL147731 46629 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 314 4 0 2 4.8 C1=C(c2ccccc2)CCN(Cc2ccn(-c3ccccc3)c2)C1 10.1021/jm00025a013
10567507 126038 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 317 4 0 3 3.8 c1ccc(N2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
CHEMBL343657 126038 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 317 4 0 3 3.8 c1ccc(N2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
60165416 82071 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL2037431 82071 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
60165416 82071 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL2037431 82071 0 None 7 8 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
44405492 147300 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 376 5 1 3 4.7 Cc1ccc(CN2CC[C@H](NC(=O)c3cccc(-c4cccs4)c3)C2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL381019 147300 0 None 15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 376 5 1 3 4.7 Cc1ccc(CN2CC[C@H](NC(=O)c3cccc(-c4cccs4)c3)C2)cc1 10.1016/j.bmcl.2005.08.051
11638780 83870 0 None 1412 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 345 3 0 5 2.8 Fc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL207488 83870 0 None 1412 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 345 3 0 5 2.8 Fc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
10044835 118183 0 None 45 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 372 7 0 4 4.1 COc1cccc(C(=O)CCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL327245 118183 0 None 45 3 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 372 7 0 4 4.1 COc1cccc(C(=O)CCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
9951233 109567 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1021/acs.jmedchem.7b00151
CHEMBL305276 109567 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 369 3 0 3 3.0 CN1C(=O)C(N2CCN(Cc3ccc(Cl)cc3)CC2)Cc2ccccc21 10.1021/acs.jmedchem.7b00151
54583898 68385 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 7 0 4 3.3 C#Cc1ccc2c(c1)CCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
CHEMBL1771114 68385 0 None -8 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 7 0 4 3.3 C#Cc1ccc2c(c1)CCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
44376569 64215 0 None 19 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL165504 64215 0 None 19 2 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 324 4 0 5 2.5 c1ccc(OC[C@H]2CC[C@H]3CN(c4ncccn4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
168286048 199701 0 None 371 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5191408 199701 0 None 371 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
CHEMBL5222229 199701 0 None 371 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1cccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)c1 10.1021/acs.jmedchem.2c00840
57396484 76944 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940417 76944 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57396484 76944 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940417 76944 2 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
56926585 75780 0 None 1000 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 358 4 0 5 2.9 COc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
CHEMBL1923293 75780 0 None 1000 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 358 4 0 5 2.9 COc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
10090130 199772 0 None 19 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 6 0 3 3.6 O=C1CCc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5199358 199772 0 None 19 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 6 0 3 3.6 O=C1CCc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5222630 199772 0 None 19 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 363 6 0 3 3.6 O=C1CCc2ccccc2N1CCCCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
44340097 16212 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL111749 16212 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10759511 213743 0 None 128 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 3 0 4 3.5 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
CHEMBL91273 213743 0 None 128 2 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 339 3 0 4 3.5 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
4826074 110881 6 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL309372 110881 6 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 322 4 1 4 2.9 COc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
9902381 126289 0 None 114 3 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
CHEMBL345552 126289 0 None 114 3 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 337 3 1 4 2.6 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1 10.1021/jm990277d
9885114 126382 5 None 47 12 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL346389 126382 5 None 47 12 Human 8.4 pKi = 8.4 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1021/jm990277d
1353 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
3559 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
86 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
CHEMBL54 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
DB00502 8692 93 None -3 85 Human 8.4 pKi = 8.4 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
10759511 213743 0 None 128 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 339 3 0 4 3.5 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL91273 213743 0 None 128 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 339 3 0 4 3.5 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1016/j.ejmech.2020.113034
9887091 114166 0 None 27 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1(C)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL317879 114166 0 None 27 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1(C)Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
10023466 171693 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 392 4 1 3 4.2 Clc1ccccc1CCN1CCN(c2[nH]nc3c2CCc2ccccc2-3)CC1 10.1021/jm0002432
CHEMBL422314 171693 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 392 4 1 3 4.2 Clc1ccccc1CCN1CCN(c2[nH]nc3c2CCc2ccccc2-3)CC1 10.1021/jm0002432
CHEMBL5290993 201298 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 301 2 1 2 3.0 CC(C)N1C[C@H](NC(=O)N2Cc3ccccc3[C@@H]2C)[C@@H](C)C1 10.1016/j.ejmech.2020.113141
9885114 126382 5 None 47 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1016/j.ejmech.2020.113141
CHEMBL346389 126382 5 None 47 12 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 357 3 1 4 3.0 O=C1COc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)ccc2N1 10.1016/j.ejmech.2020.113141
21527771 76931 1 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940404 76931 1 None -1 10 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
25139181 191121 0 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
CHEMBL484358 191121 0 None -2 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
25072941 163253 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 163253 0 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
10780942 28103 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL131396 28103 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
10805355 29172 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL132455 29172 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
118719926 122558 0 None 102 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354073 122558 0 None 102 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 358 9 1 3 3.6 O=C1CCc2ccccc2N1CCCN1CCC(CCCCCO)CC1 10.1021/acs.jmedchem.8b00265
10719212 214033 0 None 25 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 471 6 2 4 4.3 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CC4CC(C3)CC2C4)C1 10.1021/jm9601720
CHEMBL92924 214033 0 None 25 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 471 6 2 4 4.3 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@H]1CCN(C2C3CC4CC(C3)CC2C4)C1 10.1021/jm9601720
72164299 98928 5 None 9 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 321 3 0 3 3.7 Clc1cccc(N2CCN(Cc3cccnc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420780 98928 5 None 9 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 321 3 0 3 3.7 Clc1cccc(N2CCN(Cc3cccnc3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
10780942 28103 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
CHEMBL131396 28103 1 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 305 9 1 3 3.8 Clc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
10805355 29172 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL132455 29172 0 None 79 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 316 10 1 5 3.0 O=[N+]([O-])c1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
10519543 120274 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 317 3 0 3 4.1 O=c1ccc2ccc(CN3CC=C(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL332001 120274 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 317 3 0 3 4.1 O=c1ccc2ccc(CN3CC=C(c4ccccc4)CC3)cc2o1 10.1021/jm990266k
155519378 177190 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 505 11 2 5 4.7 COc1ccccc1N1CCN(CCCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4448166 177190 0 None 17 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 505 11 2 5 4.7 COc1ccccc1N1CCN(CCCCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
25072632 118553 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
CHEMBL3287392 118553 0 None -1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 418 7 0 5 4.6 Clc1cccc(N2CCN(CCCCOc3ccc4ccnn4c3)CC2)c1Cl 10.1021/jm5004039
18403576 12963 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL108122 12963 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.3 COc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
71294321 199565 0 None 512 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 351 5 0 5 2.0 O=C1CCc2ccccc2N1CCCN1CCN(c2ncccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5172871 199565 0 None 512 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 351 5 0 5 2.0 O=C1CCc2ccccc2N1CCCN1CCN(c2ncccn2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221357 199565 0 None 512 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 351 5 0 5 2.0 O=C1CCc2ccccc2N1CCCN1CCN(c2ncccn2)CC1 10.1021/acs.jmedchem.2c00840
10593869 213807 0 None 60 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 348 4 1 5 3.8 Cc1c(-c2ccccn2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL91553 213807 0 None 60 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 348 4 1 5 3.8 Cc1c(-c2ccccn2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10574303 214099 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 423 5 0 4 5.5 Cc1c(-c2ccccc2)n(-c2ccccc2)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL93432 214099 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 423 5 0 4 5.5 Cc1c(-c2ccccc2)n(-c2ccccc2)c(=O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
11451022 98931 0 None 10 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 352 5 0 4 4.6 CCOc1ccccc1N1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420890 98931 0 None 10 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 352 5 0 4 4.6 CCOc1ccccc1N1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmcl.2013.07.033
6603950 210103 9 None -13 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL64875 210103 9 None -13 8 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
3050372 76941 7 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 296 6 0 3 3.3 c1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940414 76941 7 None 5 6 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 296 6 0 3 3.3 c1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
127047996 146424 0 None 5 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797758 146424 0 None 5 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
71583848 94506 0 None 6 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336892 94506 0 None 6 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
11315028 117421 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 380 6 1 4 4.3 COc1ccc(Cl)cc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL325789 117421 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 380 6 1 4 4.3 COc1ccc(Cl)cc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
155529592 178226 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4463200 178226 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 509 10 2 5 4.4 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
71454294 90852 0 None 23 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207639 90852 0 None 23 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44340084 15860 0 None 6 4 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL109912 15860 0 None 6 4 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
10549355 212282 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 406 5 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(N)nc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
CHEMBL80722 212282 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 406 5 1 4 5.1 Cc1c(-c2ccc(Cl)cc2)nc(N)nc1C1CCN(CCc2ccccc2)CC1 10.1021/jm970111h
9948965 122147 0 None 74 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 283 9 1 2 4.0 Cc1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL334989 122147 0 None 74 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 283 9 1 2 4.0 Cc1ccc(CCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
137633863 163404 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 163404 0 None -2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
44459463 105935 0 None 19 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 1 2 4.8 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
CHEMBL281195 105935 0 None 19 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 331 4 1 2 4.8 Cc1c(C2CCN(Cc3ccccc3)CC2)n[nH]c1-c1ccccc1 10.1016/s0960-894x(99)00169-9
10020040 106744 0 None 72 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 338 4 1 4 3.6 CSc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28651 106744 0 None 72 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 338 4 1 4 3.6 CSc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
155528865 178168 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4462108 178168 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
155528865 178168 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4462108 178168 0 None 1 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 3 4.0 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cn3)CC2)cc1 10.1016/j.bmc.2020.115943
137660046 166122 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4100183 166122 0 None -6 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
71734129 97836 0 None -11 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
CHEMBL2397480 97836 0 None -11 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
1613 9127 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
205 9127 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
3964 9127 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
CHEMBL831 9127 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
DB00408 9127 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00004a016
1613 9127 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
205 9127 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
3964 9127 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
CHEMBL831 9127 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
DB00408 9127 53 None -2 44 Human 8.3 pKi = 8.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm00043a008
9839426 18922 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CCC(CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL1184179 18922 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CCC(CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL337228 18922 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.Binding affinity in humans Dopamine receptor D4 expressed in CHO cells was determined using the agonist [3H]spiperone.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CCC(CNCc1ccccc1)O2 10.1021/jm9703653
11153076 11729 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL104801 11729 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
137631542 163190 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 359 6 0 3 4.6 CCOc1ccccc1CC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/acs.jmedchem.7b00151
CHEMBL4066603 163190 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 359 6 0 3 4.6 CCOc1ccccc1CC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/acs.jmedchem.7b00151
72901200 126555 25 None 154 4 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5212743
CHEMBL3480577 126555 25 None 154 4 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a DRD4
ChEMBL 322 7 2 4 3.8 Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1 10.6019/CHEMBL5212743
3626837 214094 11 None -125 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100925m
CHEMBL93403 214094 11 None -125 4 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 373 6 1 4 2.9 COc1cccc(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100925m
10862425 123411 0 None -9 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccnn3c2)CC1 10.1021/jm025558r
CHEMBL336930 123411 0 None -9 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccnn3c2)CC1 10.1021/jm025558r
44335678 11582 0 None 35 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104155 11582 0 None 35 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccccc2F)CC1 10.1016/s0960-894x(02)00655-8
135398737 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
38 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
722 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
CHEMBL42 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
DB00363 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
135398737 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
38 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
722 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
CHEMBL42 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
DB00363 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
11058829 175424 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 417 3 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1016/j.ejmech.2020.113141
CHEMBL436274 175424 0 None 2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 minsDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO-K1 cells assessed as inhibition constant measured after 60 mins
ChEMBL 417 3 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1016/j.ejmech.2020.113141
21219166 106848 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3cnc(-c4ccccc4)c3)CC2)cc1 10.1016/s0960-894x(99)00169-9
CHEMBL287217 106848 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 317 4 0 3 4.4 c1ccc(CN2CCC(n3cnc(-c4ccccc4)c3)CC2)cc1 10.1016/s0960-894x(99)00169-9
44436608 153534 0 None -47 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL392437 153534 0 None -47 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
122181332 128651 0 None -8 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590083 128651 0 None -8 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
56833464 75171 0 None -19 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1138 38 2 16 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916720 75171 0 None -19 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1138 38 2 16 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
11230330 141965 0 None -19 3 Human 7.4 pKi = 7.4 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
CHEMBL372020 141965 0 None -19 3 Human 7.4 pKi = 7.4 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
11417804 11606 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 386 7 0 5 3.9 CCOc1cc(C#N)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104216 11606 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 386 7 0 5 3.9 CCOc1cc(C#N)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11750030 11626 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 402 5 0 4 4.8 Clc1ccc(CN2CCOC(COc3ccc(Cl)c4cccnc34)C2)cc1 10.1021/jm031111m
CHEMBL104307 11626 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 402 5 0 4 4.8 Clc1ccc(CN2CCOC(COc3ccc(Cl)c4cccnc34)C2)cc1 10.1021/jm031111m
11058829 175424 0 None 2 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL436274 175424 0 None 2 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 1 5 4.7 Clc1ccc2c(c1)C(N1CCN(CCc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
135398737 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
38 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
722 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
CHEMBL42 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
DB00363 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm401958n
49798837 21116 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1171249 21116 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200077 21116 0 None -16 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 1 3 4.5 OC1(c2ccc(I)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
10761258 107884 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.02.012
CHEMBL295094 107884 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1016/j.bmcl.2005.02.012
134130247 161354 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3890153 161354 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3991291 161354 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
11036640 127925 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL357684 127925 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
10040546 213484 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL89719 213484 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 301 1 0 1 5.0 C[C@H]1c2ccccc2C=C(C2=CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
155552695 180823 0 None -22 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 268 3 0 3 2.7 CCc1cc(Cl)c(OC)c(N2CCN(C)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4543685 180823 0 None -22 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 268 3 0 3 2.7 CCc1cc(Cl)c(OC)c(N2CCN(C)CC2)c1 10.1021/acs.jmedchem.6b00860
11407122 174592 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 406 7 0 6 3.9 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL430658 174592 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 406 7 0 6 3.9 COc1ccc([N+](=O)[O-])cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
12050201 209653 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 7 1 5 5.3 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL62624 209653 0 None -2 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 471 7 1 5 5.3 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
42626318 63010 0 None -3090 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
CHEMBL1627306 63010 0 None -3090 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in human HEK293 cell membrane for 1 hr by liquid scintillation counting analysis
ChEMBL 460 7 3 4 3.8 O=C(NCC[C@@H](O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/ml500006v
71658205 97181 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 481 9 1 5 5.3 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccc(F)cc3)s2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386619 97181 0 None -51 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 481 9 1 5 5.3 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(-c3ccc(F)cc3)s2)CC1 10.1016/j.bmc.2013.03.074
44438234 100386 2 None -19 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246644 100386 2 None -19 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 341 3 1 3 4.6 OC1(c2ccc(Cl)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
16094681 90122 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
CHEMBL219261 90122 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 343 4 1 3 2.6 Cc1cc(F)ccc1NC(=O)CN1CCC(c2cccc[n+]2[O-])CC1 10.1021/jm060662k
164609172 191186 0 None -91 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4845947 191186 0 None -91 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
127051592 147656 0 None -18 7 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818710 147656 0 None -18 7 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819742 147656 0 None -18 7 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
56594534 77375 0 None -39 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
CHEMBL1949728 77375 0 None -39 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
11036640 127925 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL357684 127925 0 None 12 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
10761258 107884 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1021/jm970021c
CHEMBL295094 107884 1 None 8 3 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1cccc(Cl)c1 10.1021/jm970021c
134130247 161354 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3890153 161354 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
CHEMBL3991291 161354 0 None -2 8 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 308 4 0 3 4.3 c1ccc2c(c1)CCN(CCCc1nc3ccccc3s1)C2 10.1016/j.bmc.2016.09.019
25070742 118559 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c12 10.1021/jm5004039
CHEMBL3287398 118559 0 None -2 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c12 10.1021/jm5004039
118709178 120125 0 None -23 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1154 32 0 17 9.5 O=C(CCc1cn(CCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3317465 120125 0 None -23 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1154 32 0 17 9.5 O=C(CCc1cn(CCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709161 120184 0 None -15 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 860 19 0 8 10.5 O=C(CCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318833 120184 0 None -15 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 860 19 0 8 10.5 O=C(CCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
137657322 166422 0 None -53 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 461 8 2 8 2.7 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4103639 166422 0 None -53 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 461 8 2 8 2.7 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc12 10.1016/j.bmc.2017.08.037
164622487 192901 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 339 4 0 4 2.8 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4871850 192901 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 339 4 0 4 2.8 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
11584858 89547 0 None -25 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 554 11 1 7 4.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
CHEMBL217981 89547 0 None -25 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 554 11 1 7 4.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
155562395 182727 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 182727 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
11545813 187973 0 None 4 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476109 187973 0 None 4 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
10617946 212297 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL80833 212297 0 None -1 3 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCCN(Cc4ccccc4)C3)[nH]n2)cc1 10.1021/jm970111h
10805797 119683 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.7 CCN(CCNc1ccccc1)Cc1ccc2ccc(=O)oc2c1 10.1021/jm990266k
CHEMBL331045 119683 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 322 7 1 4 3.7 CCN(CCNc1ccccc1)Cc1ccc2ccc(=O)oc2c1 10.1021/jm990266k
145979855 173307 0 None -18 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 405 7 2 5 3.5 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccnc3ccccc13)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4279136 173307 0 None -18 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 405 7 2 5 3.5 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccnc3ccccc13)CC2 10.1021/acsmedchemlett.8b00229
44319102 212920 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL86060 212920 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
20354789 121302 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335544 121302 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 281 5 0 2 3.5 c1ccc(CCC2CN(Cc3ccccc3)CCO2)cc1 10.1021/ml500267c
142590702 186575 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 466 8 1 3 5.7 O=C(c1ccccc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4744824 186575 0 None -1 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 466 8 1 3 5.7 O=C(c1ccccc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
22727346 19937 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 435 9 0 6 4.8 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4C)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1190866 19937 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 435 9 0 6 4.8 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4C)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL541791 19937 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 435 9 0 6 4.8 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4C)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
10597050 115973 0 None -3 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1cccc2c1CCCC2CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
CHEMBL321557 115973 0 None -3 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 398 6 0 3 5.4 COc1cccc2c1CCCC2CCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm991138z
44393372 73100 0 None -48 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 549 8 1 5 4.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3s2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL184993 73100 0 None -48 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 549 8 1 5 4.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3s2)CC1 10.1016/j.bmcl.2004.05.052
127053198 146150 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793112 146150 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 317 5 0 3 3.6 Clc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
127029390 146261 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794421 146261 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 347 6 0 4 3.6 COc1ccc(OC[C@@H]2CN(Cc3ccc(Cl)cc3)CCO2)cc1 10.1016/j.bmcl.2016.03.102
56964794 80839 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 418 3 0 5 4.8 Clc1ccc2c(c1)N=C(N1CCN(CCc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022272 80839 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 418 3 0 5 4.8 Clc1ccc2c(c1)N=C(N1CCN(CCc3ccccc3)CC1)c1cccnc1O2 10.1021/jm2013419
122189393 130026 0 None -7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613879 130026 0 None -7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
46917563 75110 0 None -58 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916551 75110 0 None -58 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
1353 8692 93 None -3 85 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
3559 8692 93 None -3 85 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
86 8692 93 None -3 85 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
CHEMBL54 8692 93 None -3 85 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
DB00502 8692 93 None -3 85 Human 7.4 pKi = 7.4 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00179-8
10761912 119094 0 None 6 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 3.5 COc1cccc(NC(=O)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL329228 119094 0 None 6 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 373 6 1 4 3.5 COc1cccc(NC(=O)CCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
10810976 214702 0 None 10 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1cccc2c1CCN(CCN1CCN(c3ccc(Cl)cc3)CC1)C2=O 10.1021/jm991138z
CHEMBL96799 214702 0 None 10 3 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 5 0 4 3.2 COc1cccc2c1CCN(CCN1CCN(c3ccc(Cl)cc3)CC1)C2=O 10.1021/jm991138z
9928335 126875 2 None -1 6 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL35093 126875 2 None -1 6 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
10520781 213764 0 None - 1 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 2 0 4 3.0 COc1ccc2c3c(c(=O)oc2c1)CN(C(=O)c1ccccc1)CC3 10.1021/jm970170v
CHEMBL91367 213764 0 None - 1 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 2 0 4 3.0 COc1ccc2c3c(c(=O)oc2c1)CN(C(=O)c1ccccc1)CC3 10.1021/jm970170v
16103 211417 47 None -5 4 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL73538 211417 47 None -5 4 Human 6.4 pKi = 6.4 Binding
Affinity was evaluated as inhibition constant for dopamine D-4 receptorAffinity was evaluated as inhibition constant for dopamine D-4 receptor
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00043a008
1438298 45393 5 None 26 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 328 5 1 3 2.9 Cc1ccc(C(=O)C2CCN(CC(=O)NC3CCCC3)CC2)cc1 10.1021/acs.jmedchem.9b01560
CHEMBL1465169 45393 5 None 26 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 328 5 1 3 2.9 Cc1ccc(C(=O)C2CCN(CC(=O)NC3CCCC3)CC2)cc1 10.1021/acs.jmedchem.9b01560
44381146 65281 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL168372 65281 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL5087504 221883 0 None -1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None Oc1cccc(C(CCNCCCCN2CCN(c3ccccc3)CC2)c2cccc(O)c2)c1 10.1021/acs.jmedchem.1c00611
17755868 149896 1 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
CHEMBL389559 149896 1 None -5 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
44330650 114179 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 212 0 1 1 3.2 Cc1ccc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317988 114179 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 212 0 1 1 3.2 Cc1ccc(C)c2c1CCCc1c[nH]nc1-2 10.1016/s0960-894x(03)00587-0
11676873 15967 0 None -1071 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
CHEMBL110365 15967 0 None -1071 6 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 455 8 1 4 4.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3c(c2)Cc2ccccc2-3)CC1 10.1021/jm0704200
122180612 128518 0 None -72 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 467 9 0 6 5.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588983 128518 0 None -72 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 467 9 0 6 5.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1016/j.bmc.2015.01.017
17755991 159077 0 None -14 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
CHEMBL396950 159077 0 None -14 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
CHEMBL5073904 221086 0 None -6 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCNCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL5269361 200378 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 359 5 1 4 3.1 Fc1ccc(OC[C@@H]2CN(Cc3ccc4[nH]cnc4c3)CCO2)cc1F 10.1016/j.ejmech.2022.114840
16744004 99103 0 None -204 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
CHEMBL243012 99103 0 None -204 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
72191068 99130 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 458 9 0 8 4.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4cnco4)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430438 99130 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 458 9 0 8 4.2 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(-c4cnco4)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL5269361 200378 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 359 5 1 4 3.1 Fc1ccc(OC[C@@H]2CN(Cc3ccc4[nH]cnc4c3)CCO2)cc1F 10.1016/j.ejmech.2022.114840
168270563 196729 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5170381 196729 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
168270563 196729 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5170381 196729 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.bmcl.2022.128615
168270563 196729 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5170381 196729 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 357 5 1 3 4.0 Fc1ccc(COC2CCN(Cc3ccc4[nH]cnc4c3)CC2)cc1F 10.1016/j.ejmech.2022.114840
9843137 11599 0 None 6 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 4 2.9 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCOc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104196 11599 0 None 6 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 4 0 4 2.9 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCOc2ccccc21 10.1016/s0960-894x(02)00655-8
71657944 97169 0 None -77 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 421 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386607 97169 0 None -77 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 421 8 1 5 4.2 COc1ccccc1N1CCCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1016/j.bmc.2013.03.074
49783209 24381 0 None -74 26 Rat 7.4 pKi = 7.4 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 24381 0 None -74 26 Rat 7.4 pKi = 7.4 Binding
Binding affinity to rat dopamine D4 receptorBinding affinity to rat dopamine D4 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
44335996 11697 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104678 11697 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
9796180 119647 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 295 6 1 4 3.0 O=c1ccc2ccc(CNCCOc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL330966 119647 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 295 6 1 4 3.0 O=c1ccc2ccc(CNCCOc3ccccc3)cc2o1 10.1021/jm990266k
93601125 146129 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
CHEMBL3792941 146129 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 343 7 0 5 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1OC 10.1016/j.bmcl.2016.03.102
44276170 103092 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 382 9 0 5 3.9 COc1cccc(C(=O)CCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
CHEMBL26135 103092 0 None -12 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 382 9 0 5 3.9 COc1cccc(C(=O)CCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/S0960-894X(97)00218-7
10001519 106085 0 None -8 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 408 8 0 4 5.1 COc1ccccc1N1CCN(CCCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL28209 106085 0 None -8 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 408 8 0 4 5.1 COc1ccccc1N1CCN(CCCCC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
44431463 94845 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234641 94845 2 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
11761412 123729 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
CHEMBL338606 123729 0 None -89 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
72737744 121296 0 None 64 3 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335538 121296 0 None 64 3 Human 7.4 pKi = 7.4 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
44408818 146943 1 None -21 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
CHEMBL380330 146943 1 None -21 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
164621388 192515 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
CHEMBL4866058 192515 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
11328099 11622 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 3.6 COc1cc(I)ccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
CHEMBL104291 11622 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 439 6 0 4 3.6 COc1cc(I)ccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
9826801 114714 0 None -18620 12 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL319352 114714 0 None -18620 12 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
57390694 77241 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946255 77241 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2012.01.022
57390694 77241 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
CHEMBL1946255 77241 0 None -1 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 385 5 0 4 5.1 Clc1ccc(N2CCCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.ejmech.2012.03.042
57403981 77270 0 None -33 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946745 77270 0 None -33 6 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
76524414 147647 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819434 147647 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819713 147647 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
44330639 214954 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 219 0 0 4 2.4 Cc1sc(C)c2c1CCCc1nncn1-2 10.1016/s0960-894x(03)00587-0
CHEMBL98331 214954 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 219 0 0 4 2.4 Cc1sc(C)c2c1CCCc1nncn1-2 10.1016/s0960-894x(03)00587-0
11488247 207418 0 None -7244 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL599487 207418 0 None -7244 4 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
71062664 153639 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ncccc1OC[C@@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL3925231 153639 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ncccc1OC[C@@H]1CN(CCN2CCc3ccccc32)CCO1 nan
168292271 198668 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5199815 198668 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
76524414 147647 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819434 147647 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819713 147647 0 None -33 8 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 426 6 1 4 5.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
46231849 208197 0 None -2754 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604732 208197 0 None -2754 4 Human 5.4 pKi = 5.4 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
9950913 109529 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 363 3 0 3 3.1 Cc1ccc(CN2CCN(C3CCc4ccccc4N(C)C3=O)CC2)cc1 10.1016/s0960-894x(00)00421-2
CHEMBL305061 109529 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 363 3 0 3 3.1 Cc1ccc(CN2CCN(C3CCc4ccccc4N(C)C3=O)CC2)cc1 10.1016/s0960-894x(00)00421-2
11794570 205524 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm970111h
CHEMBL58296 205524 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm970111h
10884046 172148 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL423735 172148 0 None -3 5 Human 7.4 pKi = 7.4 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
44403213 78562 4 None -83 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 423 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
CHEMBL196744 78562 4 None -83 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 423 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
155531809 178436 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 555 8 2 4 4.3 O=C(NCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4466114 178436 0 None 11 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 555 8 2 4 4.3 O=C(NCCN1CCN(c2ccc(I)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
162648426 186739 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 6 0 3 4.6 Fc1ccc(CCCCN2C3CCC2CN(c2ccc(Cl)cn2)C3)cc1 10.1016/j.bmc.2020.115943
CHEMBL4746695 186739 0 None 2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 6 0 3 4.6 Fc1ccc(CCCCN2C3CCC2CN(c2ccc(Cl)cn2)C3)cc1 10.1016/j.bmc.2020.115943
127053215 146202 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793858 146202 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 313 6 0 4 3.0 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
164621388 192515 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
CHEMBL4866058 192515 0 None -7 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 0 3 3.7 Clc1ccc2c(c1)CC(CCN1CCN(c3ccccn3)CC1)C2 10.1016/j.ejmech.2021.113243
44431466 94846 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234643 94846 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2ccc(Br)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
3038495 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
7625 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
CHEMBL25236 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
11794570 205524 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm960072u
CHEMBL58296 205524 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 386 4 0 3 6.0 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)on3)CC2)cc1 10.1021/jm960072u
1248739 146864 16 None 19 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 310 3 0 4 2.8 Fc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL380054 146864 16 None 19 6 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 310 3 0 4 2.8 Fc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
22100962 211046 0 None 40 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc2sc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
CHEMBL71209 211046 0 None 40 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccc2sc(C3=CCN(Cc4ccccc4)CC3)nc2c1 10.1016/S0960-894X(97)00402-2
135398737 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
38 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
722 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
CHEMBL42 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
DB00363 7745 93 None -13 90 Human 7.4 pKi = 7.4 Binding
Displacement of radiolabeled clozapine from human dopamine D4.4 receptorDisplacement of radiolabeled clozapine from human dopamine D4.4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm8007618
3038495 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
7625 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
CHEMBL25236 7495 37 None -91 18 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cellsInhibition of [3H]spiperone binding to human dopamine receptor D4.4 expressed in Chinese hamster ovary cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
242 7258 124 None -104 51 Human 7.4 pKi = 7.4 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
34 7258 124 None -104 51 Human 7.4 pKi = 7.4 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
60795 7258 124 None -104 51 Human 7.4 pKi = 7.4 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
CHEMBL1112 7258 124 None -104 51 Human 7.4 pKi = 7.4 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
DB01238 7258 124 None -104 51 Human 7.4 pKi = 7.4 Binding
Partial agonist activity at human D4 receptor assessed as inhibition constantPartial agonist activity at human D4 receptor assessed as inhibition constant
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c00704
60165541 82121 0 None 1 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 4 5.1 O=C(CCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037518 82121 0 None 1 5 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 4 5.1 O=C(CCCN1CCC(c2ccccc2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
44329749 119381 0 None -28 3 Human 7.4 pKi = 7.4 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCOC2c3cc(O)ccc3SCC21 10.1021/jm0000113
CHEMBL330216 119381 0 None -28 3 Human 7.4 pKi = 7.4 Binding
Tested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cellsTested for antagonist binding affinity by measuring displacement of [3H]spiperone from Human Dopamine receptor D4 expressed in CHO K-1 cells
ChEMBL 265 2 1 4 2.7 CCCN1CCOC2c3cc(O)ccc3SCC21 10.1021/jm0000113
164609650 191776 0 None -1 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4854456 191776 0 None -1 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
10003809 89940 0 None -97 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 448 8 1 6 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3s2)CC1 10.1021/jm0611152
CHEMBL218318 89940 0 None -97 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 448 8 1 6 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3s2)CC1 10.1021/jm0611152
137653986 165509 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 249 1 3 5 0.1 O=C1COc2c(N3CCNCC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4093493 165509 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 249 1 3 5 0.1 O=C1COc2c(N3CCNCC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
44319369 212598 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
CHEMBL83306 212598 0 None 2 4 Human 6.4 pKi = 6.4 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
168292271 198668 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
CHEMBL5199815 198668 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.bmcl.2022.128615
44381432 127496 0 None -1 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL354748 127496 0 None -1 4 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
71658208 97184 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 441 10 1 6 3.4 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc(OC)c2OC)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386622 97184 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 441 10 1 6 3.4 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc(OC)c2OC)CC1 10.1016/j.bmc.2013.03.074
168292271 198668 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
CHEMBL5199815 198668 0 None 5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 424 6 1 3 5.1 Cc1c(Cl)cccc1NC(=O)CN1CCC(OCc2ccc(Cl)c(F)c2)CC1 10.1016/j.ejmech.2022.114840
134141355 161364 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3924565 161364 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3991357 161364 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
44582675 196480 0 None -7 15 Human 6.4 pKi = 6.4 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 196480 0 None -7 15 Human 6.4 pKi = 6.4 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
76318477 113066 0 None -2454 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 422 8 3 5 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133875 113066 0 None -2454 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 422 8 3 5 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139049 113066 0 None -2454 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 422 8 3 5 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(O)ccc3[nH]2)CC1 10.1039/c3md00098b
44438226 161442 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 395 5 2 2 4.5 CC(=O)NCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL399601 161442 0 None -2 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 395 5 2 2 4.5 CC(=O)NCC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
122180573 128503 0 None -891 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 517 7 0 5 6.3 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5c(c4)Cc4ccccc4-5)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
CHEMBL3588918 128503 0 None -891 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 517 7 0 5 6.3 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5c(c4)Cc4ccccc4-5)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
134141355 161364 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3924565 161364 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3991357 161364 0 None -3 9 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.8 O=C(CCCN1CCCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
168295019 199278 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL5209079 199278 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 357 5 0 4 3.8 Fc1ccc(CO[C@H]2CCCN(Cc3ncn4ccccc34)C2)cc1F 10.1016/j.bmcl.2022.128615
44396220 132201 1 None -177 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
CHEMBL364565 132201 1 None -177 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
133633 9021 53 None -104 8 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2010.05.052
177 9021 53 None -104 8 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2010.05.052
CHEMBL445102 9021 53 None -104 8 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1016/j.bmc.2010.05.052
44278496 106325 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 8 0 3 5.2 COC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28355 106325 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 8 0 3 5.2 COC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
44278624 107120 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 409 7 1 3 5.2 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28953 107120 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 409 7 1 3 5.2 OC(COc1cccc2ccccc12)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/S0960-894X(97)00233-3
52943802 24390 0 None 7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 363 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1258270 24390 0 None 7 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 363 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
57395341 76086 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928135 76086 0 None -2 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
71583849 94507 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(-n2cc(CN3CCN(c4cc5ccc4CCc4ccc(cc4)CC5)CC3)cn2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336893 94507 0 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 448 4 0 4 5.1 c1ccc(-n2cc(CN3CCN(c4cc5ccc4CCc4ccc(cc4)CC5)CC3)cn2)cc1 10.1016/j.bmc.2013.01.065
164609650 191776 0 None -1 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4854456 191776 0 None -1 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 389 4 0 4 4.0 O=C1c2cc(Cl)c(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
6937303 209986 7 None 3 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 4.1 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)cs2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL64376 209986 7 None 3 4 Human 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 4.1 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)cs2)cc1 10.1016/s0960-894x(00)00405-4
44264742 103949 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 298 3 0 4 2.8 c1ccn2ncc(CN3CCN(C4CCCCC4)CC3)c2c1 10.1016/s0960-894x(98)00692-1
CHEMBL268190 103949 0 None 1 4 Human 5.4 pKi = 5.4 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 298 3 0 4 2.8 c1ccn2ncc(CN3CCN(C4CCCCC4)CC3)c2c1 10.1016/s0960-894x(98)00692-1
75201901 173204 19 None -331 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 173204 19 None -331 24 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
42626380 63017 0 None -125 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 548 8 3 5 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627313 63017 0 None -125 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 548 8 3 5 3.1 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3[nH]2)CC1 10.1021/jm900095y
3191 109635 97 None -10 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 109635 97 None -10 25 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
145986752 174055 0 None -1 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 174055 0 None -1 17 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
44393403 71852 0 None -125 6 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL182379 71852 0 None -125 6 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1016/j.bmcl.2004.05.052
10432808 65523 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168611 65523 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
10001207 172100 0 None 38 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL423440 172100 0 None 38 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
155514137 176607 0 None 15 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 539 9 2 4 5.0 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4439728 176607 0 None 15 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 539 9 2 4 5.0 O=C(NCCCN1CCN(c2ccc(Br)cc2)CC1)NN(Cc1ccc(F)cc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
118709179 120203 0 None -18 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1198 35 0 18 9.5 O=C(CCc1cn(CCOCCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318851 120203 0 None -18 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1198 35 0 18 9.5 O=C(CCc1cn(CCOCCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44222488 203005 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 382 7 0 4 4.5 Clc1ccc(N2CCN(CCCCCc3cc4ccccn4n3)CC2)cc1 10.1021/jm900690y
CHEMBL561622 203005 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 382 7 0 4 4.5 Clc1ccc(N2CCN(CCCCCc3cc4ccccn4n3)CC2)cc1 10.1021/jm900690y
11303390 11659 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CC(C)Oc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104476 11659 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 375 7 0 4 4.4 CC(C)Oc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
8592415 71943 6 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL182432 71943 6 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1cccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)c1 10.1016/j.bmcl.2004.07.068
10763496 118374 0 None 5 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1ccc2c(c1)C(NCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
CHEMBL328283 118374 0 None 5 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 399 6 1 4 4.1 COc1ccc2c(c1)C(NCCN1CCN(c3ccc(Cl)cc3)CC1)CCC2 10.1021/jm991138z
135471592 128460 0 None 3 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 2 5 4.8 Cc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL358657 128460 0 None 3 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 397 3 2 5 4.8 Cc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
72737728 121297 0 None 60 2 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335539 121297 0 None 60 2 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 311 6 0 3 3.5 COc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
127051592 147656 0 None -18 7 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818710 147656 0 None -18 7 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819742 147656 0 None -18 7 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 317 5 0 2 3.4 [O-][S+](CCCN1CCc2ccccc2C1)c1ccc(F)cc1 10.1016/j.bmc.2016.05.053
42606339 24703 0 None 19 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1259241 24703 0 None 19 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
44381279 65513 0 None 10 4 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL168571 65513 0 None 10 4 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cellsIn vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D4 in CHO cells
ChEMBL 348 4 1 4 2.1 O=C1C[C@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
44330638 114054 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 233 0 0 4 2.7 Cc1sc(C)c2c1CCCc1nnc(C)n1-2 10.1016/s0960-894x(03)00587-0
CHEMBL317051 114054 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 233 0 0 4 2.7 Cc1sc(C)c2c1CCCc1nnc(C)n1-2 10.1016/s0960-894x(03)00587-0
44335722 115653 0 None 7 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL321058 115653 0 None 7 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44427827 100050 0 None -1548 6 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL244990 100050 0 None -1548 6 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
44276105 20226 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 381 7 0 5 4.9 Cc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1193100 20226 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 381 7 0 5 4.9 Cc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL544451 20226 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 381 7 0 5 4.9 Cc1ccccc1N1CCN(CCCCc2cc(-c3cccs3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL5093200 222195 0 None -39 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)CCC(C(=O)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
10546828 212205 0 None 5 3 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.3 CC1(c2cc(-c3ccc(Cl)cc3)[nH]n2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
CHEMBL80207 212205 0 None 5 3 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 4 1 2 5.3 CC1(c2cc(-c3ccc(Cl)cc3)[nH]n2)CCN(Cc2ccccc2)CC1 10.1021/jm970111h
44323762 213356 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 292 3 1 3 2.9 c1ccc(CN2CCN(c3cccc4[nH]cnc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
CHEMBL88837 213356 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 292 3 1 3 2.9 c1ccc(CN2CCN(c3cccc4[nH]cnc34)CC2)cc1 10.1016/s0960-894x(98)00474-0
44323851 213753 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL91310 213753 0 None -10 4 Human 7.3 pKi = 7.3 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
76309672 92663 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 288 3 1 1 2.2 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]cnc34)cc2)cc1 10.1007/s00044-012-0055-5
CHEMBL2298811 92663 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 288 3 1 1 2.2 c1ccc(C[n+]2cc[n+](-c3cccc4[nH]cnc34)cc2)cc1 10.1007/s00044-012-0055-5
45482151 204788 0 None -9 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 451 8 1 9 1.7 COc1ccccc1N1CCN(CCNC(=O)c2cn(-c3ccc([N+](=O)[O-])cc3)nn2)CC1 10.1016/j.bmc.2009.06.041
CHEMBL573791 204788 0 None -9 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 451 8 1 9 1.7 COc1ccccc1N1CCN(CCNC(=O)c2cn(-c3ccc([N+](=O)[O-])cc3)nn2)CC1 10.1016/j.bmc.2009.06.041
9843031 116842 0 None 56 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL323537 116842 0 None 56 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCc2ccccc21 10.1016/s0960-894x(02)00655-8
44380815 65784 0 None 2 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL169193 65784 0 None 2 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
11299620 104059 3 None -87 5 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL269004 104059 3 None -87 5 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/jm960345l
127032086 146100 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
CHEMBL3792637 146100 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 337 5 0 5 2.9 Cn1ncc2cc(CN3CCO[C@H](COc4ccccc4)C3)ccc21 10.1016/j.bmcl.2016.03.102
127030606 146140 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793033 146140 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
90644226 118556 0 None -22 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287395 118556 0 None -22 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
122181328 128647 0 None -33 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 449 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590079 128647 0 None -33 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 449 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2cc(F)c(F)c(F)c2)CC1 10.1016/j.bmc.2014.12.012
135398737 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
38 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
722 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
CHEMBL42 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
DB00363 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00108-5
11033734 16493 1 None -120 6 Human 7.3 pKi = 7.3 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@H]1c1ccccc1C2 10.1021/jm010566d
CHEMBL113238 16493 1 None -120 6 Human 7.3 pKi = 7.3 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)C[C@H]1c1ccccc1C2 10.1021/jm010566d
164609529 191243 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4846823 191243 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
76336022 113156 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115581 113156 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139316 113156 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 386 6 1 5 3.3 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(OCCF)cc3)CC1)CC2 10.1021/jm401384w
11304676 109583 0 None 8 2 Human 7.3 pKi = 7.3 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 418 6 1 4 3.3 COc1cc(Br)cc(C(=O)NCCN2CCc3ccccc3C2)c1OC 10.1016/j.bmcl.2003.09.083
CHEMBL305366 109583 0 None 8 2 Human 7.3 pKi = 7.3 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 418 6 1 4 3.3 COc1cc(Br)cc(C(=O)NCCN2CCc3ccccc3C2)c1OC 10.1016/j.bmcl.2003.09.083
10587140 211813 1 None 1 3 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 255 3 1 2 3.1 Cc1cc(C2CCN(Cc3ccccc3)CC2)[nH]n1 10.1021/jm970111h
CHEMBL77015 211813 1 None 1 3 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 255 3 1 2 3.1 Cc1cc(C2CCN(Cc3ccccc3)CC2)[nH]n1 10.1021/jm970111h
137643132 164829 0 None -3890 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
CHEMBL4085920 164829 0 None -3890 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
164609172 191186 0 None -91 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4845947 191186 0 None -91 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 378 6 1 5 2.8 O=C1CCc2cc(C(=O)CCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
10454026 24679 0 None -1479 8 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL125916 24679 0 None -1479 8 Human 6.3 pKi = 6.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
168275515 197284 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5179340 197284 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
168275515 197284 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5179340 197284 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
168275515 197284 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5179340 197284 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 371 5 0 4 4.1 Cc1nc(CN2CCC(OCc3ccc(F)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
2726 7706 68 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 7706 68 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 7706 68 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 7706 68 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 7706 68 None -8 72 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
9886340 12186 0 None 97 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
CHEMBL107229 12186 0 None 97 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1cccc2c1N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
44380816 127129 0 None 22 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL353090 127129 0 None 22 4 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
6604756 105607 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL278751 105607 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
6604756 105607 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1021/jm00073a021
CHEMBL278751 105607 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone Binding towards dopamine receptor D4 expressed in CHO-K1 cells using [3H]spiperone
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1021/jm00073a021
164609529 191243 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
CHEMBL4846823 191243 0 None -64 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 5 0 4 4.1 CC1(CCCN2CCN(c3ccccn3)CC2)Cc2cc(Cl)ccc2C1=O 10.1016/j.ejmech.2021.113243
57390116 76073 0 None -77 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928122 76073 0 None -77 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
11732013 47583 0 None 12 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 395 1 1 5 4.8 Clc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148559 47583 0 None 12 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 395 1 1 5 4.8 Clc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
6604756 105607 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(97)10068-3
CHEMBL278751 105607 18 None -8 7 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(97)10068-3
72190766 99135 0 None -12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL2430443 99135 0 None -12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
10831786 212302 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.5 Clc1ccc(-c2cc(C3CCCCN3Cc3ccccc3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL80863 212302 0 None -2 3 Human 5.3 pKi = 5.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.5 Clc1ccc(-c2cc(C3CCCCN3Cc3ccccc3)[nH]n2)cc1 10.1021/jm970111h
156016177 184433 0 None -47 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1ccc2nc(N)sc2c1-3 10.1016/j.bmc.2020.115578
CHEMBL4641502 184433 0 None -47 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-N-Methylspiperone from human dopamine D4 receptor expressed in stable HEK cells incubated for 90 mins by microbeta counting method
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1ccc2nc(N)sc2c1-3 10.1016/j.bmc.2020.115578
16744005 150656 0 None -23 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
CHEMBL390181 150656 0 None -23 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 535 10 0 6 5.7 COc1ccc(C2=NO[C@@H](CCCN3CCN(C(c4ccc(F)cc4)c4ccc(F)cc4)CC3)C2)cc1OC 10.1016/j.ejmech.2006.12.030
46231782 207282 0 None -2089 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL598730 207282 0 None -2089 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
44415704 86934 0 None -1659 6 Human 5.3 pKi = 5.3 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213424 86934 0 None -1659 6 Human 5.3 pKi = 5.3 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
10242548 32376 40 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 4 1 2 2.6 CCCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL135152 32376 40 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 219 4 1 2 2.6 CCCNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
118719792 122497 0 None -97 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.4 COc1ccccc1N1CCN(CCCCc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3353895 122497 0 None -97 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 391 8 0 6 3.4 COc1ccccc1N1CCN(CCCCc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmc.2015.01.017
21171 193755 33 None -8 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL490533 193755 33 None -8 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hrDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
56589561 77376 0 None -53 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
CHEMBL1949729 77376 0 None -53 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
13091358 77230 0 None -12 6 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946122 77230 0 None -12 6 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
9845181 214940 3 None -34 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
CHEMBL98241 214940 3 None -34 13 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
13091356 120315 0 None -12 8 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321789 120315 0 None -12 8 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 6 1 3 4.8 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCOc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
44276155 106268 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 437 8 1 5 3.5 COc1ccccc1N1CCN(CCCNC(=O)C2CCCc3cccc(OC)c32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL283211 106268 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 437 8 1 5 3.5 COc1ccccc1N1CCN(CCCNC(=O)C2CCCc3cccc(OC)c32)CC1 10.1016/S0960-894X(97)00218-7
72164180 98920 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1cccc(N2CCN(Cc3cccs3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420772 98920 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1cccc(N2CCN(Cc3cccs3)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
118709165 120188 0 None -22 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 916 23 0 8 12.1 O=C(CCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318837 120188 0 None -22 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 916 23 0 8 12.1 O=C(CCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709167 120190 0 None -5 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 972 27 0 8 13.6 O=C(CCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318839 120190 0 None -5 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 972 27 0 8 13.6 O=C(CCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
25141534 63009 0 None -1698 7 Human 5.3 pKi = 5.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627305 63009 0 None -1698 7 Human 5.3 pKi = 5.3 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
146025727 178464 0 None -181 27 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 178464 0 None -181 27 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
11016418 112899 0 None -7943 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL313424 112899 0 None -7943 9 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
137645196 164737 0 None -117 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 277 1 2 5 0.9 CN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4084712 164737 0 None -117 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 277 1 2 5 0.9 CN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
49798855 21082 0 None -234 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 375 3 0 4 3.7 CN1CN(c2ccccc2)C2(CCN(Cc3coc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1169896 21082 0 None -234 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 375 3 0 4 3.7 CN1CN(c2ccccc2)C2(CCN(Cc3coc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
CHEMBL1199933 21082 0 None -234 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 375 3 0 4 3.7 CN1CN(c2ccccc2)C2(CCN(Cc3coc4ccccc34)CC2)C1=O 10.1016/j.bmc.2010.05.052
10597114 178628 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 400 4 1 3 5.0 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL446892 178628 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 400 4 1 3 5.0 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
71061585 167276 0 None -3 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 367 6 0 5 2.8 Cc1ccnc(C)c1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL4112090 167276 0 None -3 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 367 6 0 5 2.8 Cc1ccnc(C)c1OC[C@H]1CN(CCN2CCc3ccccc32)CCO1 nan
CHEMBL4752561 220817 0 None -3 2 Human 5.3 pKi = 5.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000739a DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000739a DRD4
ChEMBL None None None COc1cc(-c2cn([C@H]3CCc4ccccc4N(CC(F)(F)F)C3=O)nn2)ccc1-n1ccc(C)n1 10.6019/CHEMBL5212743
164619236 192488 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4865591 192488 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
10551026 108394 0 None 1 5 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL298875 108394 0 None 1 5 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
9821803 134244 0 None 524 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 390 5 1 2 5.0 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL366043 134244 0 None 524 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 390 5 1 2 5.0 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2004.07.045
131396 213514 6 None 1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
CHEMBL89934 213514 6 None 1 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Dopamine receptor D4.2 in CHO cellsBinding affinity against human Dopamine receptor D4.2 in CHO cells
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm960268u
10641783 49453 0 None 354 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL150129 49453 0 None 354 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 353 4 1 5 2.3 COc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
9820304 108846 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1016/s0960-894x(00)00421-2
CHEMBL1204116 108846 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1016/s0960-894x(00)00421-2
CHEMBL302075 108846 0 None 12 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)c(Cl)c1 10.1016/s0960-894x(00)00421-2
1353 8692 93 None -3 85 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
3559 8692 93 None -3 85 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
86 8692 93 None -3 85 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
CHEMBL54 8692 93 None -3 85 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
DB00502 8692 93 None -3 85 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(02)00656-x
44336047 11557 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104058 11557 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00656-x
44335925 11717 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104751 11717 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 413 5 0 4 3.4 COc1ccc(Cl)cc1CN1CCN(CC(=O)N2c3ccccc3C[C@H]2C)CC1 10.1016/s0960-894x(02)00656-x
44335835 11847 0 None 1174 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 3.8 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105454 11847 0 None 1174 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 3.8 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00656-x
9867233 12273 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 5 0 5 2.6 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL107631 12273 0 None 234 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 427 5 0 5 2.6 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
9865490 174728 0 None 53 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 395 5 0 3 3.6 C=C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL431640 174728 0 None 53 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 395 5 0 3 3.6 C=C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
44335795 11773 0 None 33 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1cccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
CHEMBL105011 11773 0 None 33 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 362 4 0 2 4.6 Cc1cccc(CN2CCC(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
44335816 11989 0 None 758 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(OC(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106208 11989 0 None 758 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(OC(F)(F)F)cc2)CC1 10.1016/s0960-894x(02)00655-8
10157556 127013 0 None 21 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
CHEMBL352207 127013 0 None 21 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 395 3 0 3 3.4 O=C1C(N2CCN(Cc3ccc(Cl)cc3)CC2)CCc2cccc3c2N1CC3 10.1016/s0960-894x(02)01056-9
127031515 146212 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL3793910 146212 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.ejmech.2022.114840
1353 8692 93 None -3 85 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
3559 8692 93 None -3 85 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
86 8692 93 None -3 85 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
CHEMBL54 8692 93 None -3 85 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
DB00502 8692 93 None -3 85 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
11668034 140305 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccc(F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL370823 140305 0 None 2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 380 5 1 3 4.6 O=C(N[C@H]1CCN(Cc2ccc(F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
22100940 210733 4 None 112 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 306 3 0 3 4.6 C1=C(c2nc3ccccc3s2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
CHEMBL69355 210733 4 None 112 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 306 3 0 3 4.6 C1=C(c2nc3ccccc3s2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
19958507 106197 0 None 81 4 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 320 4 1 3 3.4 CCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL282829 106197 0 None 81 4 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 320 4 1 3 3.4 CCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
10715375 206480 0 None 630 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 4.9 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL59326 206480 0 None 630 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 4.9 COc1cc2ccccc2cc1C(=O)OCC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
10525119 86514 6 None 79 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 401 5 1 3 3.8 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
CHEMBL21168 86514 6 None 79 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 401 5 1 3 3.8 O=C(NCCN1CCN(c2ccc(Cl)cc2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/0960-894X(96)00198-9
127031515 146212 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL3793910 146212 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.ejmech.2022.114840
76325156 113167 1 None -7 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 113167 1 None -7 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 113167 1 None -7 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
10049549 90041 0 None 537 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 452 3 0 4 3.9 Clc1ccc(N2CCN(Cc3cnn4c(I)cccc34)CC2)cc1 10.1021/jm0611152
CHEMBL218787 90041 0 None 537 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 452 3 0 4 3.9 Clc1ccc(N2CCN(Cc3cnn4c(I)cccc34)CC2)cc1 10.1021/jm0611152
9968343 49513 0 None 169 3 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
CHEMBL150181 49513 0 None 169 3 Human 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)NC(=O)CO4)CC2)cc1C 10.1021/jm990277d
155563452 182088 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4573441 182088 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
145967572 171712 0 None 1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4224763 171712 0 None 1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
72545238 99902 0 None 25 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443005 99902 0 None 25 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
155563452 182088 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL4573441 182088 0 None 6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 361 6 0 4 3.7 O=C(CCCN1CCN(c2ccc(Cl)cn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
10643589 214247 0 None 13 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2cccc(Cl)c2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL94283 214247 0 None 13 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 381 4 1 4 5.1 Cc1c(-c2cccc(Cl)c2)nc(O)n1C1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
3691783 11536 1 None 47 3 Human 8.3 pKi = 8.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL103871 11536 1 None 47 3 Human 8.3 pKi = 8.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 10.1021/jm960637m
11797442 113803 0 None 32 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL315446 113803 0 None 32 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
127031832 146193 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3793782 146193 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 340 5 1 3 3.6 Fc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
16759175 61768 21 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
CHEMBL1334895 61768 21 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
CHEMBL1616116 61768 21 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constantDisplacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 280 3 1 4 2.7 Cc1ncc(CN2CC=C(c3ccccc3)CC2)c(N)n1 10.1016/j.ejmech.2020.113141
137651073 164247 0 None 2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4079301 164247 0 None 2 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
10360923 98326 2 None 831 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(C#N)c2)CC1 10.1016/s0960-894x(99)00169-9
CHEMBL24052 98326 2 None 831 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 356 4 0 4 4.6 Cc1c(-c2ccccc2)cnn1C1CCN(Cc2cccc(C#N)c2)CC1 10.1016/s0960-894x(99)00169-9
10737474 108130 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL296953 108130 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
9975465 194430 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49502 194430 0 None 109 3 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2005.02.012
137661377 165988 0 None 173 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL4098720 165988 0 None 173 8 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 314 6 0 2 3.9 CCCC1CCN(CCCN2C(=O)CCc3ccccc32)CC1 10.1021/acs.jmedchem.8b00265
44412191 145153 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1021/jm0611152
CHEMBL377200 145153 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1021/jm0611152
10737474 108130 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
CHEMBL296953 108130 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1021/jm970021c
13091268 84999 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL210578 84999 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
13091268 84999 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
CHEMBL210578 84999 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Binding affinity to human cloned dopamine D4.4 receptor by radioligand binding assayBinding affinity to human cloned dopamine D4.4 receptor by radioligand binding assay
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2006.03.057
13091268 84999 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL210578 84999 0 None -8 14 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
25071691 118564 0 None -9 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 118564 0 None -9 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
44412191 145153 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1016/j.bmcl.2006.02.075
CHEMBL377200 145153 0 None 60 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1016/j.bmcl.2006.02.075
71734031 97835 0 None -21 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
CHEMBL2397479 97835 0 None -21 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
10133031 64312 0 None 38 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 358 4 0 3 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(F)cc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
CHEMBL166321 64312 0 None 38 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement.
ChEMBL 358 4 0 3 3.9 Fc1ccc(OC[C@@H]2CC[C@H]3CN(c4ccc(F)cc4)CCN3C2)cc1 10.1016/s0960-894x(98)00108-5
10518406 25650 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL128276 25650 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1016/j.bmcl.2005.02.012
10518406 25650 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
CHEMBL128276 25650 0 None 69 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 301 10 1 4 3.1 COc1ccc(OCCNCCCOc2ccccc2)cc1 10.1021/jm970422s
9952003 12132 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106916 12132 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
10000302 214000 0 None 741 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
CHEMBL92713 214000 0 None 741 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm020952a
127031831 146118 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
CHEMBL3792805 146118 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 352 6 1 4 3.5 COc1ccc2c(CN3CCO[C@H](COc4ccccc4)C3)c[nH]c2c1 10.1016/j.bmcl.2016.03.102
11504230 84992 0 None -12 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL210567 84992 0 None -12 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
53364153 70615 0 None 3 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 929 25 0 16 7.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCCCCCCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803023 70615 0 None 3 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 929 25 0 16 7.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCCCCCCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
11233944 11555 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 366 5 2 4 4.0 Oc1cc(Cl)ccc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104041 11555 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 366 5 2 4 4.0 Oc1cc(Cl)ccc1NCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
10000302 214000 0 None 741 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
CHEMBL92713 214000 0 None 741 2 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.In vitro binding affinity at human Dopamine receptor D4.4 by [3H]YM-09151-2 displacement.
ChEMBL 387 7 1 4 3.3 COc1cccc(C(=O)NCCCN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1021/jm991138z
10760638 194955 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL49876 194955 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2005.02.012
57396571 76940 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940413 76940 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
10618874 209925 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL6416 209925 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
10667201 118169 0 None 60 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 375 6 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCCc2ccccc2)CC1 10.1021/jm991029k
CHEMBL327176 118169 0 None 60 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 375 6 1 4 4.8 Cc1c(-c2ccccc2)nc(O)n1C1CCN(CCCc2ccccc2)CC1 10.1021/jm991029k
10546453 118479 0 None 27 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 360 4 2 3 4.0 O=C(Nc1nccc2ccccc12)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
CHEMBL328667 118479 0 None 27 3 Human 8.3 pKi = 8.3 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 360 4 2 3 4.0 O=C(Nc1nccc2ccccc12)NC1CCN(Cc2ccccc2)CC1 10.1021/jm991029k
10760638 194955 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
CHEMBL49876 194955 0 None 131 3 Human 8.3 pKi = 8.3 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 354 4 1 4 2.7 N#Cc1ccccc1N1CCN(CNC(=O)c2ccc(Cl)cc2)CC1 10.1021/jm970021c
10618874 209925 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm0002432
CHEMBL6416 209925 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm0002432
168280742 197863 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity to human D4R in transfected cellsCompetitive binding affinity to human D4R in transfected cells
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187578 197863 0 None -1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity to human D4R in transfected cellsCompetitive binding affinity to human D4R in transfected cells
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
145969667 171744 0 None -1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 171744 0 None -1 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
10618874 209925 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm960072u
CHEMBL6416 209925 0 None 95 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 365 5 1 2 5.2 Clc1ccc(-c2cc(C3CCN(CCc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm960072u
11774177 12155 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 407 6 0 4 4.9 CC(=O)c1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL107068 12155 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 407 6 0 4 4.9 CC(=O)c1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL4513786 220746 7 None 34 8 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
CHEMBL4796803 220746 7 None 34 8 Human 8.3 pKi = 8.3 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000289bCl DRD4
ChEMBL None None None CCCCN(CCCC)C(=O)CN1C[C@@H](c2cc(OC)c3c(c2)OCO3)[C@H](C(=O)O)[C@H]1CC(C)(C)CCC 10.6019/CHEMBL5212743
10693793 114478 0 None 33 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL319079 114478 0 None 33 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 427 7 2 4 3.7 COc1cc(NC(=O)C2CC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
10758004 28183 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
CHEMBL131484 28183 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1021/jm970422s
57396571 76940 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940413 76940 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57396571 76940 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940413 76940 0 None 3 5 Rat 8.3 pKi = 8.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 330 6 0 3 3.9 Clc1ccc(N2CCN(CCCOc3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
19964410 166477 1 None 70 3 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 322 5 1 3 3.4 c1ccc(OCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL4104272 166477 1 None 70 3 Human 8.3 pKi = 8.3 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 322 5 1 3 3.4 c1ccc(OCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
10758004 28183 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL131484 28183 0 None 31 3 Human 8.3 pKi = 8.3 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 319 9 1 3 4.1 Cc1ccc(OCCCNCCOc2ccc(Cl)cc2)cc1 10.1016/j.bmcl.2005.02.012
6466372 176841 12 None 93 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4443054 176841 12 None 93 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 311 4 1 5 1.5 Cc1cccc(NC(=O)CN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
15467371 107784 0 None 912 4 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL294458 107784 0 None 912 4 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
45482152 204789 0 None 20 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 517 9 1 8 3.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn(-c2ccc([N+](=O)[O-])cc2)nn1 10.1016/j.bmc.2009.06.041
CHEMBL573792 204789 0 None 20 4 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4.4 expressed in CHO cellsBinding affinity to human cloned dopamine D4.4 expressed in CHO cells
ChEMBL 517 9 1 8 3.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn(-c2ccc([N+](=O)[O-])cc2)nn1 10.1016/j.bmc.2009.06.041
57401706 76946 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940419 76946 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57401706 76946 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940419 76946 0 None 1 11 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
25071692 118566 0 None -13 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 118566 0 None -13 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
76325156 113167 1 None -7 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 113167 1 None -7 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 113167 1 None -7 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
44364166 47587 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 280 5 2 4 3.3 O=c1ccc2ccc(NCCNc3ccccc3)cc2o1 10.1021/jm0002432
CHEMBL148561 47587 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 280 5 2 4 3.3 O=c1ccc2ccc(NCCNc3ccccc3)cc2o1 10.1021/jm0002432
9926143 120303 1 None 74 4 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
CHEMBL332154 120303 1 None 74 4 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 294 6 2 4 3.0 O=c1ccc2ccc(CNCCNc3ccccc3)cc2o1 10.1021/jm990266k
127031515 146212 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
CHEMBL3793910 146212 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 331 6 0 4 3.1 COc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1F 10.1016/j.bmcl.2022.128615
145969667 171744 0 None -1 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 171744 0 None -1 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
52919 21222 48 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL1200986 21222 48 None -3 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
71733932 97827 0 None -25 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
CHEMBL2397389 97827 0 None -25 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
10378194 204544 0 None 45 6 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL57176 204544 0 None 45 6 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
155523515 177644 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 567 11 2 5 5.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(-c3ccccc3)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4454096 177644 0 None 12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 567 11 2 5 5.9 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(-c3ccccc3)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
155555060 181104 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1cccc(CN(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c2ccc(F)cc2)c1 10.1021/acs.jmedchem.9b01085
CHEMBL4550633 181104 0 None 14 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1cccc(CN(NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)c2ccc(F)cc2)c1 10.1021/acs.jmedchem.9b01085
1353 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
3559 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
86 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
CHEMBL54 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
DB00502 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
44278479 169921 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 0 2 5.6 c1ccc(CC2CCN(CCCOc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL417858 169921 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 359 7 0 2 5.6 c1ccc(CC2CCN(CCCOc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
135887934 18104 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 379 7 1 6 3.1 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL1179502 18104 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 379 7 1 6 3.1 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
CHEMBL80627 18104 0 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 379 7 1 6 3.1 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)nc1 10.1016/S0960-894X(97)00442-3
10084583 111555 4 None -93 6 Human 7.3 pKi = 7.3 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 111555 4 None -93 6 Human 7.3 pKi = 7.3 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 50/2200)
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
10639430 175948 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4cnccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL440511 175948 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 320 4 1 5 2.2 c1ccc(-c2nc(CN3CCN(c4cnccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
135398745 9688 112 None -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
47 9688 112 None -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
CHEMBL715 9688 112 None -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
DB00334 9688 112 None -10 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
44454707 104607 0 None 21 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
CHEMBL272073 104607 0 None 21 5 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
44335987 11585 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 4 0 3 4.8 CC1CC(C)(C)N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104160 11585 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 4 0 3 4.8 CC1CC(C)(C)N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
132578545 161337 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3898250 161337 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991133 161337 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
135398745 9688 112 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
47 9688 112 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
CHEMBL715 9688 112 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
DB00334 9688 112 None -7 65 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
10663221 40487 1 None 60 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4)CC3)c2c1 10.1021/jm0009989
CHEMBL142217 40487 1 None 60 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4)CC3)c2c1 10.1021/jm0009989
22727323 19913 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 436 9 0 7 4.4 COc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1190607 19913 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 436 9 0 7 4.4 COc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL541270 19913 0 None -8 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 436 9 0 7 4.4 COc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
44270444 56098 0 None 138 4 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
CHEMBL156369 56098 0 None 138 4 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
44273882 85003 0 None 79 2 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 385 6 1 3 3.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL21059 85003 0 None 79 2 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 385 6 1 3 3.8 CC(C)(C)C(=O)NCCCCN1CCN(c2ccc(C(F)(F)F)cc2)CC1 10.1016/0960-894X(96)00198-9
10939222 211181 1 None -100 5 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperoneBinding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperone
ChEMBL 445 8 1 4 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(Br)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL71960 211181 1 None -100 5 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperoneBinding affinity towards Chinese hamster ovary cells transfected with human D4 receptor using [3H]spiperone
ChEMBL 445 8 1 4 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(Br)cc2)CC1 10.1016/0960-894X(95)00011-H
132578545 161337 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3898250 161337 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
CHEMBL3991133 161337 0 None -104 9 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 325 3 0 2 4.1 O=C1c2ccc(Cl)cc2CC1CCN1CCc2ccccc2C1 10.1016/j.bmc.2016.09.019
2865 10915 73 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
59 10915 73 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
60854 10915 73 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
CHEMBL708 10915 73 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
DB00246 10915 73 None -66 53 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm070516u
44340415 15350 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL109472 15350 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
44340302 16524 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL113471 16524 0 None 1 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44332686 215203 0 None -44 4 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 320 8 2 4 2.2 CS(=O)(=O)Nc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
CHEMBL99849 215203 0 None -44 4 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 320 8 2 4 2.2 CS(=O)(=O)Nc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
CHEMBL5267339 200299 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 340 5 1 5 3.1 Clc1ccc(-n2cc(CNC[C@@H]3CCCOC3)nn2)c(Cl)c1 10.1016/j.ejmech.2020.113141
130431290 180814 0 None -436 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 417 9 2 4 3.5 CCc1c[nH]c(C(=O)NCCCCN2CCN(c3cccc(CC)c3Cl)CC2)n1 10.1021/acs.jmedchem.6b00860
CHEMBL4543524 180814 0 None -436 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 417 9 2 4 3.5 CCc1c[nH]c(C(=O)NCCCCN2CCN(c3cccc(CC)c3Cl)CC2)n1 10.1021/acs.jmedchem.6b00860
72545009 99899 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443002 99899 0 None -1 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
11659604 145352 0 None 30 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4ccncc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL377542 145352 0 None 30 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4ccncc4n3)CC2)cc1 10.1021/jm060166w
10034684 76182 69 None 18 2 Human 6.3 pKi = 6.3 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
CHEMBL19331 76182 69 None 18 2 Human 6.3 pKi = 6.3 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 135 0 2 2 1.4 Oc1ccc2c(c1)CCN2 10.1016/S0960-894X(97)00194-7
155568411 182859 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4591118 182859 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 331 4 1 5 1.9 O=C(CN1CCN(c2ccc(Cl)cn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
137647533 164732 0 None -81 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 477 7 2 7 3.8 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4084690 164732 0 None -81 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 477 7 2 7 3.8 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
11154555 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
164619236 192488 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
CHEMBL4865591 192488 0 None -25 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 366 6 1 5 2.6 O=C1CCc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc2N1 10.1016/j.ejmech.2021.113243
154704705 183104 1 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4590356 183104 1 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595409 183104 1 None -2 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL5074399 221095 0 None -19 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCCCNCCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
130431336 181687 0 None -389 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 401 7 2 4 3.0 CCc1cccc(N2CCN(C/C=C/CNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4564507 181687 0 None -389 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 401 7 2 4 3.0 CCc1cccc(N2CCN(C/C=C/CNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
71062579 155009 0 None - 1 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cn1 nan
CHEMBL3936182 155009 0 None - 1 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 353 6 0 5 2.5 Cc1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cn1 nan
44427970 159389 0 None -9 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL397207 159389 0 None -9 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
11269330 208272 0 None -16595 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605127 208272 0 None -16595 4 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
44330637 214953 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 198 0 0 2 2.6 Cn1cc2c(n1)-c1ccccc1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL98330 214953 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 198 0 0 2 2.6 Cn1cc2c(n1)-c1ccccc1CCC2 10.1016/s0960-894x(03)00587-0
11154555 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 7587 62 None -501 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
16744171 99332 0 None -245 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
CHEMBL243224 99332 0 None -245 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 453 10 0 7 4.2 CCOc1ccccc1N1CCN(CCC[C@@H]2CC(c3ccc(OC)c(OC)c3)=NO2)CC1 10.1016/j.ejmech.2006.12.030
57345620 77269 0 None -32 3 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1[C@H]2CC[C@@H]1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
CHEMBL1946744 77269 0 None -32 3 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1[C@H]2CC[C@@H]1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2012.01.022
76518515 147648 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3818881 147648 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819714 147648 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
13373172 206562 0 None -125 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL593897 206562 0 None -125 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
44335721 114080 0 None 50 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(F)cc21 10.1016/s0960-894x(02)00655-8
CHEMBL317266 114080 0 None 50 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 387 4 0 3 3.2 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(F)cc21 10.1016/s0960-894x(02)00655-8
127030909 146259 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3794375 146259 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 367 6 0 4 3.9 FC(F)(F)Oc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
57402787 75970 0 None -14 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1926700 75970 0 None -14 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
44276111 19682 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 450 10 0 7 4.8 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1189040 19682 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 450 10 0 7 4.8 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL537975 19682 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 450 10 0 7 4.8 CCOc1ccccc1N1CCN(CCCCc2cc(-c3cccc([N+](=O)[O-])c3)no2)CC1 10.1016/s0960-894x(02)00179-8
10247720 19826 1 None 2 5 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 19826 1 None 2 5 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 19826 1 None 2 5 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
60165543 82122 0 None 1 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 6 0 7 2.9 O=C(CCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037519 82122 0 None 1 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 6 0 7 2.9 O=C(CCCN1CCN(c2ncccn2)CC1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
9881815 213447 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]cnc23)cc1 10.1016/s0960-894x(99)00434-5
CHEMBL89420 213447 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 267 6 2 3 2.7 c1ccc(CNCCOc2cccc3[nH]cnc23)cc1 10.1016/s0960-894x(99)00434-5
242 7258 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
34 7258 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
60795 7258 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
CHEMBL1112 7258 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
DB01238 7258 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2020.115943
122180574 128504 0 None -512 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 468 7 1 5 5.2 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5[nH]ccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
CHEMBL3588919 128504 0 None -512 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 468 7 1 5 5.2 Clc1cccc(N2CCN(CCCCc3cn(-c4ccc5[nH]ccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.01.017
154725277 183211 1 None -19 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4472900 183211 1 None -19 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596220 183211 1 None -19 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
242 7258 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
34 7258 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
60795 7258 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
CHEMBL1112 7258 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
DB01238 7258 124 None -104 51 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2021.113243
242 7258 124 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
34 7258 124 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
60795 7258 124 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
CHEMBL1112 7258 124 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
DB01238 7258 124 None -87 51 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2016.05.053
135501649 126544 0 None 5 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 1 2 5 3.2 Cc1ccc2c(c1)C(NC1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL347959 126544 0 None 5 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 321 1 2 5 3.2 Cc1ccc2c(c1)C(NC1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm0104825
71449034 85198 0 None 3 4 Human 6.3 pKi = 6.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111526 85198 0 None 3 4 Human 6.3 pKi = 6.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
60165545 82130 0 None -2 4 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 336 6 0 4 4.7 O=C(CCCCN1Cc2ccccc2C1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
CHEMBL2037527 82130 0 None -2 4 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 336 6 0 4 4.7 O=C(CCCCN1Cc2ccccc2C1)c1nc2ccccc2s1 10.1016/j.ejmech.2012.03.042
76518515 147648 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3818881 147648 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
CHEMBL3819714 147648 0 None -31 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 454 7 1 5 5.8 O=C(CCCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1nc2ccccc2s1 10.1016/j.bmc.2016.06.011
44456400 19606 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 19606 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 19606 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 19606 0 None -21 10 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
44591088 196361 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL514591 196361 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
44438236 161679 2 None -173 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
CHEMBL400827 161679 2 None -173 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 354 3 1 3 4.3 Cn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
100 10577 58 None -8 54 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 10577 58 None -8 54 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 10577 58 None -8 54 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 10577 58 None -8 54 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 10577 58 None -8 54 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
10806501 212062 0 None 24 2 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccncc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL79098 212062 0 None 24 2 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 332 5 1 3 3.9 c1ccc(CCN2CCC(c3cc(-c4ccncc4)[nH]n3)CC2)cc1 10.1021/jm970111h
9857248 211883 6 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77708 211883 6 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 292 3 1 3 2.9 c1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
44278458 106466 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 7 1 3 4.8 Cc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL28458 106466 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 389 7 1 3 4.8 Cc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
136072267 19945 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 378 7 1 5 3.7 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL1190896 19945 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 378 7 1 5 3.7 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
CHEMBL541826 19945 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 378 7 1 5 3.7 c1ccc(N2CCN(CCCCCNC3=Nc4ccccc4OC3)CC2)cc1 10.1016/S0960-894X(97)00442-3
23992579 98919 5 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420771 98919 5 None 8 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 292 3 0 3 3.7 Clc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
3251 10844 58 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
5684 10844 58 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
80 10844 58 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL31354 10844 58 None -43 12 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
44405445 142555 0 None 9 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
CHEMBL373032 142555 0 None 9 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2005.08.051
11280787 115993 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 391 9 0 5 3.6 COCCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL321701 115993 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 391 9 0 5 3.6 COCCOc1ccccc1OCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
12899569 73398 0 None -20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 393 7 1 5 3.1 COc1ccccc1N1CCN(CCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1813597 73398 0 None -20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 393 7 1 5 3.1 COc1ccccc1N1CCN(CCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
CHEMBL1852735 73398 0 None -20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 393 7 1 5 3.1 COc1ccccc1N1CCN(CCCOc2ccc3ccc(=O)[nH]c3c2)CC1 10.1016/j.bmc.2011.04.021
11375068 168637 1 None -588 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccnc2)cc1 10.1021/jm049465g
CHEMBL414838 168637 1 None -588 3 Human 6.3 pKi = 6.3 Binding
Binding affinity for human dopamine D4 receptorBinding affinity for human dopamine D4 receptor
ChEMBL 480 7 1 4 5.2 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2cccnc2)cc1 10.1021/jm049465g
44578446 188359 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476934 188359 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
118709164 120187 0 None -87 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 902 22 0 8 11.7 O=C(CCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318836 120187 0 None -87 4 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 902 22 0 8 11.7 O=C(CCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44335998 13237 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 5 0 4 2.9 O=C1COc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL108261 13237 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 385 5 0 4 2.9 O=C1COc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
71657945 97170 0 None -58 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 10 1 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386608 97170 0 None -58 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 427 10 1 4 3.9 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmc.2013.03.074
109030515 182764 1 None 12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4588808 182764 1 None 12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 325 5 1 5 1.9 Cc1cccc(NC(=O)CCN2CCN(c3ncccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
10803828 18355 1 None -2630 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL1180609 18355 1 None -2630 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
CHEMBL135044 18355 1 None -2630 5 Human 6.3 pKi = 6.3 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 295 2 1 3 3.1 Oc1ccc2c(c1)O[C@@H](CN1CCc3ccccc3C1)CC2 10.1021/jm9703653
130431340 178124 0 None -851 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 403 8 2 4 3.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4461461 178124 0 None -851 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 403 8 2 4 3.3 CCc1cccc(N2CCN(CCCCNC(=O)c3nc(C)c[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
130431342 176363 0 None -144 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 485 9 2 6 4.0 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4436025 176363 0 None -144 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 485 9 2 6 4.0 CCc1cc(Cl)c(OC)c(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
12050200 108867 0 None 43 4 Human 7.3 pKi = 7.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 6 1 4 4.6 c1ccc(CN2CCC(NCc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL302186 108867 0 None 43 4 Human 7.3 pKi = 7.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 363 6 1 4 4.6 c1ccc(CN2CCC(NCc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
2 10035 23 None -2 28 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
54562 10035 23 None -2 28 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
CHEMBL240773 10035 23 None -2 28 Human 7.3 pKi = 7.3 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinityIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/s0960-894x(01)00484-x
2 10035 23 None -2 28 Human 7.3 pKi = 7.3 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
54562 10035 23 None -2 28 Human 7.3 pKi = 7.3 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
CHEMBL240773 10035 23 None -2 28 Human 7.3 pKi = 7.3 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
2 10035 23 None -2 28 Human 7.3 pKi = 7.3 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
54562 10035 23 None -2 28 Human 7.3 pKi = 7.3 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
CHEMBL240773 10035 23 None -2 28 Human 7.3 pKi = 7.3 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
11772242 173066 0 None 4 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
CHEMBL427048 173066 0 None 4 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1021/jm060279f
49799687 21163 0 None -14 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 432 3 2 2 4.3 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1173285 21163 0 None -14 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 432 3 2 2 4.3 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200269 21163 0 None -14 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 432 3 2 2 4.3 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
135398737 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
38 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
722 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
CHEMBL42 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
DB00363 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
Cataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar testCataleptogenic effect against cloned human dopamine receptor D4 in male Sprague-Dawley rats in a bar test
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
44340186 16432 0 None 8 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
CHEMBL112831 16432 0 None 8 4 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
11005852 210647 0 None -104 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 521 8 1 4 5.9 O=C(NCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
CHEMBL68720 210647 0 None -104 4 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 521 8 1 4 5.9 O=C(NCCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc2c1-c1ccccc1C2=O 10.1021/jm010146o
72191066 99132 0 None -199 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 406 8 1 7 3.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(N)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430440 99132 0 None -199 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 406 8 1 7 3.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc(N)cc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
53248209 68765 4 None -3548 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 463 7 1 4 5.0 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm200288r
CHEMBL1774386 68765 4 None -3548 4 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]-IABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 463 7 1 4 5.0 O=C(NCCC(F)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm200288r
4189 213701 96 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 213701 96 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 213701 96 None -33 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
71061785 167275 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL4112056 167275 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
10039198 63123 0 None -4 4 Human 7.3 pKi = 7.3 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 63123 0 None -4 4 Human 7.3 pKi = 7.3 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
135398737 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
38 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
722 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL42 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00363 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
1240 15595 17 None -57 4 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL109684 15595 17 None -57 4 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL1256754 15595 17 None -57 4 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
10403092 31904 4 None -26 3 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL134747 31904 4 None -26 3 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
145968810 171817 0 None -5 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 171817 0 None -5 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in stable HEK cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
44431478 94354 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL233580 94354 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 378 4 1 2 4.9 O=C(NC1CCN(Cc2cccc(Cl)c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
137657153 166336 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4102616 166336 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
135398737 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
38 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
722 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
CHEMBL42 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
DB00363 7745 93 None -13 90 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss miceIn vitro ability to inhibit the binding of [3H]spiperone to cloned human dopamine receptor D4 using apomorphine induced climbing test in male Swiss mice
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2003.07.015
10425450 6989 30 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
3301 6989 30 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
CHEMBL375596 6989 30 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/acs.jmedchem.9b00231
44393775 73078 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
CHEMBL184853 73078 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 490 4 1 4 4.2 Cc1cc(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)ccc1Br 10.1016/j.bmcl.2004.07.068
57393634 76094 0 None -48 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928248 76094 0 None -48 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
127045854 146342 0 None -416 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3797205 146342 0 None -416 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
44337725 115315 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 319 2 0 2 4.3 CN1C2CCC1CC(OC1c3ccccc3Cc3ccccc31)C2 10.1021/jm010146o
CHEMBL320114 115315 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 319 2 0 2 4.3 CN1C2CCC1CC(OC1c3ccccc3Cc3ccccc31)C2 10.1021/jm010146o
22727334 19718 4 None -30 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 361 7 0 4 4.5 c1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1189290 19718 4 None -30 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 361 7 0 4 4.5 c1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL538474 19718 4 None -30 3 Human 6.3 pKi = 6.3 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 361 7 0 4 4.5 c1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
44455426 161928 0 None -7 12 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 161928 0 None -7 12 Human 6.3 pKi = 6.3 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
10402378 72899 0 None -301 5 Human 6.3 pKi = 6.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
CHEMBL184049 72899 0 None -301 5 Human 6.3 pKi = 6.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
CHEMBL5080654 221477 0 None -8709 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2CCc1ccccc1 10.1021/acs.jmedchem.1c00611
44336127 116058 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 5 0 3 4.1 CC(C)C1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL321871 116058 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 411 5 0 3 4.1 CC(C)C1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
71455083 88605 0 None -239 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164354 88605 0 None -239 7 Human 7.3 pKi = 7.3 Binding
Binding affinity to dopamine D4 receptor by radioligand binding assayBinding affinity to dopamine D4 receptor by radioligand binding assay
ChEMBL 389 6 0 3 4.8 O=C(C1CCCCC1)N(CCN1CC=C(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
10873318 52321 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 411 10 1 5 3.4 COc1cccc(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
CHEMBL152869 52321 0 None -12 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 411 10 1 5 3.4 COc1cccc(C(=O)NCCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1021/jm020952a
2407 10145 76 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
59227 10145 76 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
941 10145 76 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
CHEMBL1303 10145 76 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
DB05271 10145 76 None -30 7 Human 7.3 pKi = 7.3 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm960345l
127047859 146829 0 None -19 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800341 146829 0 None -19 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137635685 162784 0 None -1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
CHEMBL4061986 162784 0 None -1 6 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
44326256 174915 0 None -2 4 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 285 5 0 2 5.0 CCCN(CCC)[C@@H]1CCc2c(ccc3ccoc23)[C@@H]1C 10.1016/S0960-894X(97)10068-3
CHEMBL433002 174915 0 None -2 4 Human 7.3 pKi = 7.3 Binding
Tested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cellsTested in vitro for the inhibition of [3H]spiperone binding to Dopamine receptor D4, expressed in cloned CHO cells
ChEMBL 285 5 0 2 5.0 CCCN(CCC)[C@@H]1CCc2c(ccc3ccoc23)[C@@H]1C 10.1016/S0960-894X(97)10068-3
44393411 72867 0 None -123 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 587 7 1 4 6.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL183871 72867 0 None -123 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cellsBinding affinity towards human D4.4 receptor using [3H]spiperone expressed in CHO cells
ChEMBL 587 7 1 4 6.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2s1 10.1016/j.bmcl.2004.05.052
71455082 88603 0 None -15 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1cccc2ccccc12)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164352 88603 0 None -15 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1cccc2ccccc12)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
11477180 9848 6 None -616 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
6675 9848 6 None -616 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
CHEMBL180010 9848 6 None -616 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 480 7 1 4 5.2 O=C(c1ccc(cc1)c1ccccn1)NC/C=C/CN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
857428 38596 32 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 296 4 1 2 4.5 Cc1cccc2cc(CNCc3ccccc3)c(Cl)nc12 10.1021/acs.jmedchem.9b01560
CHEMBL1406529 38596 32 None 2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting methodDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 296 4 1 2 4.5 Cc1cccc2cc(CNCc3ccccc3)c(Cl)nc12 10.1021/acs.jmedchem.9b01560
107930 8311 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
3304 8311 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
CHEMBL298406 8311 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
DB12273 8311 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
130431316 177460 0 None -13803 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4451683 177460 0 None -13803 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
107930 8311 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
3304 8311 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
CHEMBL298406 8311 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
DB12273 8311 26 None -3090 6 Human 5.3 pKi = 5.3 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
71062560 160207 0 None 1 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 352 5 0 4 2.4 O=C(CN1CCO[C@H](COc2ccccc2)C1)N1CCc2ccccc21 nan
CHEMBL3979116 160207 0 None 1 2 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 352 5 0 4 2.4 O=C(CN1CCO[C@H](COc2ccccc2)C1)N1CCc2ccccc21 nan
154703541 183078 1 None -23 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4541924 183078 1 None -23 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595195 183078 1 None -23 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
1164 8411 26 None -346 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
1626 8411 26 None -346 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
3345 8411 26 None -346 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL596 8411 26 None -346 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
DB00813 8411 26 None -346 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL 336 6 0 2 4.1 CCC(=O)N(c1ccccc1)C1CCN(CC1)CCc1ccccc1 10.1021/acs.jmedchem.1c00611
CHEMBL5279686 200814 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 358 5 0 7 2.6 Cc1csc(OC[C@@H]2CN(Cc3ccc4c(cnn4C)c3)CCO2)n1 10.1016/j.ejmech.2022.114840
9842859 212234 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 0 7 2.4 CN(CCCCN1CCN(c2ncccn2)CC1)C1=Nc2ccccc2OC1 10.1016/S0960-894X(97)00442-3
CHEMBL80411 212234 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligandBinding affinity at cloned human D4 dopamine receptor in CHO cells using [3H]-YM 09151 as radioligand
ChEMBL 380 6 0 7 2.4 CN(CCCCN1CCN(c2ncccn2)CC1)C1=Nc2ccccc2OC1 10.1016/S0960-894X(97)00442-3
1621 9207 17 None -64 44 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 9207 17 None -64 44 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 9207 17 None -64 44 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 9207 17 None -64 44 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 9207 17 None -64 44 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
22065962 183575 0 None 20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 10.1016/j.bmc.2008.12.054
CHEMBL460644 183575 0 None 20 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 10.1016/j.bmc.2008.12.054
132075278 169423 0 None 5 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
CHEMBL4169752 169423 0 None 5 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 308 3 0 3 3.1 c1ccc(CN2CCc3cc(N4CCOCC4)ccc3C2)cc1 10.1016/j.ejmech.2018.02.024
11036641 38552 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL140612 38552 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
71462265 88604 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 438 6 0 6 3.5 O=C(c1cnc2ccccc2n1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164353 88604 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 438 6 0 6 3.5 O=C(c1cnc2ccccc2n1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
145989012 174085 0 None -95 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1ccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)cc1 10.1021/acsmedchemlett.8b00229
CHEMBL4293886 174085 0 None -95 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 384 8 2 5 3.0 COc1ccc(C(=O)NCCCCN2CCc3cc(OC)c(O)cc3C2)cc1 10.1021/acsmedchemlett.8b00229
137654511 165582 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 259 1 2 4 1.0 CN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4094407 165582 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 259 1 2 4 1.0 CN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
CHEMBL5279686 200814 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 358 5 0 7 2.6 Cc1csc(OC[C@@H]2CN(Cc3ccc4c(cnn4C)c3)CCO2)n1 10.1016/j.ejmech.2022.114840
CHEMBL5075014 221133 0 None -5 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None O=C(NCCCCN1CC[C@]2(c3cccc(O)c3)CCC[C@H]1[C@@H]2O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
76311271 113065 0 None -371 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 556 17 2 7 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCOCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3133862 113065 0 None -371 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 556 17 2 7 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCOCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
CHEMBL3139046 113065 0 None -371 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assayDisplacement of [125I]ABN from human D4 receptor transfected in HEK-293 cell membrane after 60 mins by filtration binding assay
ChEMBL 556 17 2 7 3.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(OCCOCCOCCF)ccc3[nH]2)CC1 10.1039/c3md00098b
11646648 100475 8 None -102 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 5 2 4 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(SC)cc4)CC3)c2c1 10.1016/j.bmcl.2006.10.076
CHEMBL247058 100475 8 None -102 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 382 5 2 4 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(SC)cc4)CC3)c2c1 10.1016/j.bmcl.2006.10.076
681 8247 72 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 8247 72 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 8247 72 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 8247 72 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 8247 72 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
763194 98918 6 None 33 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420770 98918 6 None 33 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 276 3 0 3 3.2 Fc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
164609519 191230 0 None -47 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4846574 191230 0 None -47 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
25071384 118558 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287397 118558 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
242 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
34 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
60795 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
CHEMBL1112 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
DB01238 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm501512b
242 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
34 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
60795 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
CHEMBL1112 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
DB01238 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm0611152
44419060 144635 0 None -13 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 432 8 1 6 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3o2)CC1 10.1021/jm0611152
CHEMBL376020 144635 0 None -13 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 432 8 1 6 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(C#N)ccc3o2)CC1 10.1021/jm0611152
10684789 15984 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
CHEMBL110489 15984 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
30438 204931 33 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm9600712
CHEMBL57478 204931 33 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm9600712
30438 204931 33 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm0002432
CHEMBL57478 204931 33 None 9 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 228 2 1 1 3.4 CC1CCN(Cc2c[nH]c3ccccc23)CC1 10.1021/jm0002432
107995 103901 20 None -1380 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
29982233 103901 20 None -1380 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
CHEMBL267723 103901 20 None -1380 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
118709169 120193 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1029 31 0 8 15.2 O=C(CCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318841 120193 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1029 31 0 8 15.2 O=C(CCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10917953 214767 0 None -16595 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL97242 214767 0 None -16595 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
134154069 161226 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3970299 161226 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990113 161226 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
9980998 37808 0 None -524 7 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 37808 0 None -524 7 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 37808 0 None -524 7 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D2L receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
44335948 174704 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 3 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL431437 174704 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 3 0 3 3.4 CC1Cc2ccccc2N1C(=O)CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
154726353 183102 1 None -50 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4577162 183102 1 None -50 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595382 183102 1 None -50 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
154726792 183363 1 None -141 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4475406 183363 1 None -141 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597530 183363 1 None -141 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
10684789 15984 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL110489 15984 1 None -89 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1ccncc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
134154069 161226 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3970299 161226 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
CHEMBL3990113 161226 0 None -38 9 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 356 5 0 3 5.3 Clc1ccc2sc(CCCCN3CCc4ccccc4C3)nc2c1 10.1016/j.bmc.2016.09.019
168287735 198583 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5198353 198583 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
164617626 192239 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4861794 192239 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
164617626 192239 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
CHEMBL4861794 192239 0 None -21 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 324 6 1 5 2.4 Nc1ccc(C(=O)CCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.ejmech.2021.113243
53324045 63845 0 None -1 16 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644980 63845 0 None -1 16 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
22727332 20515 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 8 0 4 5.1 Fc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1195194 20515 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 8 0 4 5.1 Fc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL554016 20515 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 405 8 0 4 5.1 Fc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
11615489 76218 1 None -3 4 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
CHEMBL193337 76218 1 None -3 4 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm0503805
11356479 78612 0 None -8 3 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
CHEMBL196928 78612 0 None -8 3 Human 7.2 pKi = 7.2 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 221 5 0 3 2.3 CCCN(CCC)C1CCn2nccc2C1 10.1021/jm0503805
168287735 198583 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
CHEMBL5198353 198583 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.ejmech.2022.114840
168287735 198583 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
CHEMBL5198353 198583 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 373 5 1 3 4.5 Fc1cc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)ccc1Cl 10.1016/j.bmcl.2022.128615
135995891 209739 0 None 9 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 413 4 1 5 4.1 Oc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL62996 209739 0 None 9 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 413 4 1 5 4.1 Oc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
44456400 19606 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL1188501 19606 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL2436555 19606 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
CHEMBL536539 19606 0 None -21 10 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysisDisplacement of [3H]N-methylspiperone from dopamine D4 receptor (unknown origin) after 90 mins by scintillation counting analysis
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2013.08.072
16759249 16779 1 None -16 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 385 7 0 2 5.9 CCCCN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2 10.1021/acs.jmedchem.6b01373
CHEMBL11493 16779 1 None -16 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 385 7 0 2 5.9 CCCCN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2 10.1021/acs.jmedchem.6b01373
44591087 182529 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
CHEMBL458342 182529 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
11464115 75409 0 None 2 2 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
CHEMBL191815 75409 0 None 2 2 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 413 6 1 3 4.5 O=C(NCCCCN1CCN2c3ccccc3CC[C@@H]2C1)c1ccc2ccccc2c1 10.1021/jm049031l
122180576 128506 0 None -107 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
CHEMBL3588921 128506 0 None -107 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 479 8 0 6 5.1 COc1ccccc1N1CCN(CCCCn2cc(-c3ccc4c(c3)Cc3ccccc3-4)nn2)CC1 10.1016/j.bmc.2015.01.017
46231925 208157 0 None -3235 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL604525 208157 0 None -3235 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
121304441 159163 0 None -11481 5 Human 5.2 pKi = 5.2 Binding
Activity at dopamine D4 receptor (unknown origin)Activity at dopamine D4 receptor (unknown origin)
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL3970323 159163 0 None -11481 5 Human 5.2 pKi = 5.2 Binding
Activity at dopamine D4 receptor (unknown origin)Activity at dopamine D4 receptor (unknown origin)
ChEMBL 515 8 1 6 5.0 Cn1c(SCCCN2CC[C@]3(C[C@@H]3c3ccc(C(F)(F)F)cc3)C2)nnc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b00972
CHEMBL5090215 222028 0 None -389 4 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CN(C)C(=O)C(CCNCCCCN1CCc2ccc(C#N)cc2C1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
44339984 174576 0 None 10 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL430522 174576 0 None 10 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44370009 56751 0 None 10 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1c[nH]c2nc(CN3CCc4ccccc4C3)cc-2c1 10.1016/s0960-894x(99)00025-6
CHEMBL156896 56751 0 None 10 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1c[nH]c2nc(CN3CCc4ccccc4C3)cc-2c1 10.1016/s0960-894x(99)00025-6
3428803 107266 3 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 370 8 1 5 3.3 O=[N+]([O-])c1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL29098 107266 3 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 370 8 1 5 3.3 O=[N+]([O-])c1ccc(OCC(O)CN2CCC(Cc3ccccc3)CC2)cc1 10.1016/S0960-894X(97)00233-3
44307552 109118 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/s0960-894x(00)00421-2
CHEMBL303692 109118 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1016/s0960-894x(00)00421-2
44336085 11951 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 4 4.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCSc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL106007 11951 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 415 4 0 4 4.0 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCSc2ccccc21 10.1016/s0960-894x(02)00655-8
9840797 22312 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 338 3 0 4 3.3 O=c1ccc2ccc(CN3CCN(c4ccc(F)cc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL121884 22312 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 338 3 0 4 3.3 O=c1ccc2ccc(CN3CCN(c4ccc(F)cc4)CC3)cc2o1 10.1021/jm990266k
127027237 146164 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793264 146164 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 314 6 0 5 2.4 COc1ccc(CN2CCO[C@H](COc3cccnc3)C2)cc1 10.1016/j.bmcl.2016.03.102
137657951 166343 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 263 1 2 5 0.5 CN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4102646 166343 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 263 1 2 5 0.5 CN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
73353534 97833 0 None -13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
CHEMBL2397477 97833 0 None -13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
52937776 67944 0 None -83 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765629 67944 0 None -83 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2nccc2C1 10.1021/jm101639t
44307552 109118 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/acs.jmedchem.7b00151
CHEMBL303692 109118 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 357 5 0 3 3.1 CN(C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1)c1ccccc1 10.1021/acs.jmedchem.7b00151
42606573 24618 0 None 20 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1258999 24618 0 None 20 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptorDisplacement of [3H]Spiperone from human dopamine D4.4 receptor
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
12050196 209897 6 None 8 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 349 5 0 4 4.1 c1ccc(CN2CCN(Cc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL64043 209897 6 None 8 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 349 5 0 4 4.1 c1ccc(CN2CCN(Cc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
12050193 209975 0 None -1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL64325 209975 0 None -1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 443 5 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
46231846 208118 0 None -2344 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604316 208118 0 None -2344 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10735463 168655 0 None 239 3 Human 8.2 pKi = 8.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 334 4 1 5 2.5 Cc1[nH]c(-c2ccccc2)nc1CN1CCN(c2ncccn2)CC1 10.1021/jm960637m
CHEMBL415014 168655 0 None 239 3 Human 8.2 pKi = 8.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 334 4 1 5 2.5 Cc1[nH]c(-c2ccccc2)nc1CN1CCN(c2ncccn2)CC1 10.1021/jm960637m
44335877 11632 0 None 426 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)c(Cl)cc2F)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL104323 11632 0 None 426 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 419 4 0 3 3.7 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(F)c(Cl)cc2F)CC1 10.1016/s0960-894x(02)00656-x
44336027 11878 0 None 165 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105601 11878 0 None 165 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 367 4 0 3 2.9 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00656-x
44335960 13300 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL108282 13300 0 None 31 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00656-x
44336108 12456 0 None 85 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.8 CCC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL107793 12456 0 None 85 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 5 0 3 3.8 CCC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335923 115970 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
CHEMBL321538 115970 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 5 0 3 3.3 CCc1ccc(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)cc1 10.1016/s0960-894x(02)00655-8
44335884 170156 0 None 11 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL419356 170156 0 None 11 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335799 170233 0 None 102 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL419908 170233 0 None 102 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 433 5 0 4 3.7 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(OC(F)(F)F)c2)CC1 10.1016/s0960-894x(02)00655-8
1353 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
3559 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
86 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
CHEMBL54 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
DB00502 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
25071691 118564 0 None -9 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 118564 0 None -9 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL4547253 220775 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None Fc1ccc(CN2CCC(n3cc(Cc4ccc(Br)cc4)nn3)CC2)cc1 10.1016/j.bmc.2022.116851
CHEMBL4567314 220794 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL None None None Brc1ccc(Cc2cn(C3CCN(Cc4ccccc4)CC3)nn2)cc1 10.1016/j.bmc.2022.116851
71459761 90855 0 None 14 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207642 90855 0 None 14 7 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
10570563 24802 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/acs.jmedchem.7b00151
CHEMBL1202212 24802 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/acs.jmedchem.7b00151
CHEMBL126429 24802 0 None 15 2 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 360 4 0 2 4.9 Clc1ccc(N2CCN(C[C@H]3C[C@@H]3c3ccccc3)CC2)cc1Cl 10.1021/acs.jmedchem.7b00151
1353 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
3559 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
86 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
CHEMBL54 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
DB00502 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0611152
9836900 48474 1 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2cc(CN3CCN(c4ccccc4)CC3)ccc2N1 10.1021/jm990277d
CHEMBL149233 48474 1 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 323 3 1 4 2.3 O=C1COc2cc(CN3CCN(c4ccccc4)CC3)ccc2N1 10.1021/jm990277d
44336012 115991 0 None 120 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL321698 115991 0 None 120 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 383 4 0 3 3.4 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cccc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
90644058 118806 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289642 118806 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
54585811 68384 0 None -4 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 418 7 0 5 3.2 COc1ccccc1N1CCN(CCCCN2CCc3cc(C#N)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771113 68384 0 None -4 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 418 7 0 5 3.2 COc1ccccc1N1CCN(CCCCN2CCc3cc(C#N)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
90644058 118806 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289642 118806 0 None 104 4 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
2389 10104 118 None -22 66 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
5073 10104 118 None -22 66 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
96 10104 118 None -22 66 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
CHEMBL85 10104 118 None -22 66 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
DB00734 10104 118 None -22 66 Human 8.2 pKi = 8.2 Binding
Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.Binding affinity measured at the Dopamine receptor D4 by the inhibition of [3H]spiperone binding to human recombinant CHO cells using unlabeled haloperidol for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
72164302 98936 0 None 19 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 359 3 1 2 4.8 Clc1cccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420895 98936 0 None 19 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 359 3 1 2 4.8 Clc1cccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)c1Cl 10.1016/j.bmcl.2013.07.033
155562328 182622 0 None 7 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2cccc(F)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4585384 182622 0 None 7 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 521 11 2 6 4.3 COc1ccc(N(Cc2cccc(F)c2)NC(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1021/acs.jmedchem.9b01085
57393083 76942 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940415 76942 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
57393083 76942 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940415 76942 0 None 1 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2011.12.019
681 8247 72 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
940 8247 72 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
947 8247 72 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
CHEMBL59 8247 72 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
DB00988 8247 72 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm800895v
19964401 163425 0 None 208 3 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 5 1 2 4.0 c1ccc(CCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL4069306 163425 0 None 208 3 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 320 5 1 2 4.0 c1ccc(CCC2CN(Cc3c[nH]c4ccccc34)CCO2)cc1 10.1021/acs.jmedchem.7b00151
11849778 87917 0 None 35 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
CHEMBL215705 87917 0 None 35 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 360 6 0 5 2.9 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cc(F)cc(F)c1 10.1021/jm060279f
1353 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
3559 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
86 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
CHEMBL54 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
DB00502 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
1353 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
3559 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
86 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
CHEMBL54 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
DB00502 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
9817253 113332 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 283 6 3 4 2.4 Oc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL314174 113332 0 None -6 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 283 6 3 4 2.4 Oc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
10249755 174963 0 None 1258 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 5.1 COc1cc2ccccc2cc1OC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
CHEMBL433255 174963 0 None 1258 2 Human 8.2 pKi = 8.2 Binding
Binding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligandBinding affinity against cloned human Dopamine receptor D4 using [3H]nemonapride as radioligand
ChEMBL 389 6 0 4 5.1 COc1cc2ccccc2cc1OC(=O)CC1CCN(Cc2ccccc2)CC1 10.1021/jm960017l
15443 124588 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL340211 124588 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
15443 124588 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
CHEMBL340211 124588 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
1353 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
3559 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
86 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
CHEMBL54 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
DB00502 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm070516u
11336814 86876 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
CHEMBL213164 86876 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 342 6 0 5 2.8 CO/N=C(/CCN1CCN(c2ccccn2)CC1)c1cccc(F)c1 10.1021/jm060279f
11200205 145689 0 None 9 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
CHEMBL378324 145689 0 None 9 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 392 6 0 5 4.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(Cl)c(Cl)c1 10.1021/jm060279f
53363200 70627 0 None 2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 0 9 3.7 CCOCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803052 70627 0 None 2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 509 14 0 9 3.7 CCOCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
16121920 202654 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 380 5 1 6 2.7 COc1ccccc1N1CCN(Cc2c(C)[nH]c3nc(N(C)C)ncc23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL558838 202654 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 380 5 1 6 2.7 COc1ccccc1N1CCN(Cc2c(C)[nH]c3nc(N(C)C)ncc23)CC1 10.1016/j.bmc.2009.05.015
45267435 202770 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1nccc2c(CN3CCN(c4ccccc4)CC3)c[nH]c12 10.1016/j.bmc.2009.05.015
CHEMBL559868 202770 0 None 426 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 326 3 1 3 3.5 Clc1nccc2c(CN3CCN(c4ccccc4)CC3)c[nH]c12 10.1016/j.bmc.2009.05.015
10088259 108690 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL300956 108690 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1016/j.bmcl.2005.02.012
71458040 85662 0 None 27 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.5 C1=C(/C=C/c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
CHEMBL2112913 85662 0 None 27 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 329 5 1 2 4.5 C1=C(/C=C/c2ccccc2)CCN(CCc2c[nH]c3ncccc23)C1 10.1016/s0960-894x(99)00025-6
10088259 108690 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
CHEMBL300956 108690 3 None 134 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 Cc1ccc(C(=O)NCN2CCN(c3ccccc3C#N)CC2)cc1 10.1021/jm970021c
155561496 182451 0 None -5 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranesDisplacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranes
ChEMBL 438 8 0 6 3.1 COc1cc2c(cc1OC)C(=O)N(CCCCN1CCN(c3ccccn3)CC1)CCC2 10.1021/acs.jmedchem.8b00760
CHEMBL4581645 182451 0 None -5 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranesDisplacement of [3H]-N-methylspiperone from dopamine D4 receptor (unknown origin) expressed in HEK293 cell membranes
ChEMBL 438 8 0 6 3.1 COc1cc2c(cc1OC)C(=O)N(CCCCN1CCN(c3ccccn3)CC1)CCC2 10.1021/acs.jmedchem.8b00760
10065083 38877 1 None -1 10 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
CHEMBL140872 38877 1 None -1 10 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2011.12.019
137638973 163653 0 None -15 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 163653 0 None -15 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
10065083 38877 1 None 1 10 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL140872 38877 1 None 1 10 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
11653679 187970 1 None 3 11 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476108 187970 1 None 3 11 Human 8.2 pKi = 8.2 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
168273039 199575 0 None 1659 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5175009 199575 0 None 1659 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221414 199575 0 None 1659 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 394 6 0 5 3.1 O=C1CCc2ccccc2N1CCCN1CCN(c2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.2c00840
10498196 48756 0 None 63 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
CHEMBL149497 48756 0 None 63 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 352 4 1 4 3.4 COc1ccc(C2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1 10.1021/jm990277d
10382581 108075 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
CHEMBL296506 108075 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1021/jm970021c
15443 124588 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
CHEMBL340211 124588 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2020.115943
15443 124588 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
CHEMBL340211 124588 96 None 1 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 10.1016/j.ejmech.2021.113243
44278114 106981 0 None 104 3 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 334 5 1 3 3.8 CCCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
CHEMBL28833 106981 0 None 104 3 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperoneIn vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone
ChEMBL 334 5 1 3 3.8 CCCc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/s0960-894x(01)00241-4
10382581 108075 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL296506 108075 0 None 151 3 Human 8.2 pKi = 8.2 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2cccc(C)c2)CC1 10.1016/j.bmcl.2005.02.012
133079 10410 42 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm0002432
980 10410 42 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm0002432
CHEMBL69759 10410 42 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm0002432
11465618 109175 23 None -25 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 109175 23 None -25 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 109175 23 None -25 19 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]methyl-spiperone from recombinant human D4.4 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
53364225 70619 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 932 25 0 18 5.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCOCCOCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803027 70619 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 932 25 0 18 5.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCOCCOCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
10336538 8406 50 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
974 8406 50 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
CHEMBL310843 8406 50 None -3 8 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cellsDisplacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm900690y
155562395 182727 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
CHEMBL4587925 182727 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 4 1 3 3.5 Cc1ccc(C2CCN(CC(=O)Nc3cccc(C)c3)CC2)nc1 10.1021/acs.jmedchem.9b00231
9946469 50896 0 None 11 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
CHEMBL151533 50896 0 None 11 3 Human 8.2 pKi = 8.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 351 3 1 4 3.0 Cc1ccc(N2CCN(Cc3ccc4c(c3)OCC(=O)N4)CC2)cc1C 10.1021/jm990277d
9907332 23168 1 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
CHEMBL123031 23168 1 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 368 3 0 4 4.1 Cc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1Cl 10.1021/jm990266k
57391307 76938 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940411 76938 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57391307 76938 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940411 76938 0 None 8 7 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
168277064 199617 0 None 1202 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5178868 199617 0 None 1202 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
CHEMBL5221670 199617 0 None 1202 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 379 6 0 4 3.2 COc1ccc(N2CCN(CCCN3C(=O)CCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.2c00840
10786367 211955 0 None 9 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4cccc(Cl)c4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL78287 211955 0 None 9 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(-c2cc(C3CCN(Cc4cccc(Cl)c4)CC3)[nH]n2)cc1 10.1021/jm970111h
10018480 20602 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 313 3 0 1 5.0 C=CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1195797 20602 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 313 3 0 1 5.0 C=CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL555362 20602 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 313 3 0 1 5.0 C=CCN1CC=C(C2=Cc3ccccc3Cc3ccccc32)CC1 10.1021/jm00004a016
135398737 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
38 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
722 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
CHEMBL42 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
DB00363 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 dopamine receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2012.08.011
135398737 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
38 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
722 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
CHEMBL42 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
DB00363 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.ejmech.2013.05.027
137636066 163012 0 None -38 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064742 163012 0 None -38 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
71733932 97827 0 None -25 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2397389 97827 0 None -25 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
13457126 106599 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 392 6 1 4 3.9 O=C(CCN1CCN(c2ccc(CO)c(Cl)c2)CC1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00252-2
CHEMBL285543 106599 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 392 6 1 4 3.9 O=C(CCN1CCN(c2ccc(CO)c(Cl)c2)CC1)c1ccc(Cl)cc1 10.1016/s0960-894x(98)00252-2
69432471 116623 0 None -60 5 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 378 5 0 3 4.4 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCC3)c1ccc(F)cc1 10.1021/jm401958n
CHEMBL3233427 116623 0 None -60 5 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 378 5 0 3 4.4 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCC3)c1ccc(F)cc1 10.1021/jm401958n
17755867 92884 1 None -28 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
CHEMBL231070 92884 1 None -28 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
46912547 21164 0 None -67 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1173287 21164 0 None -67 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1200270 21164 0 None -67 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 462 4 2 3 4.3 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(I)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
164628178 193126 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 193126 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
10007017 89803 0 None -812 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 522 7 2 3 5.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2[nH]1 10.1021/jm0611152
CHEMBL218150 89803 0 None -812 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 522 7 2 3 5.6 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(Br)ccc2[nH]1 10.1021/jm0611152
12581154 32251 12 None -4 3 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 2 1 2 1.8 CNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL135048 32251 12 None -4 3 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 2 1 2 1.8 CNC1CCc2c(cccc2OC)C1 10.1021/jm960345l
10184153 20076 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 477 10 0 4 6.6 C(=C/c1cc(CCCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL1191883 20076 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 477 10 0 4 6.6 C(=C/c1cc(CCCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
CHEMBL543041 20076 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 477 10 0 4 6.6 C(=C/c1cc(CCCCN2CCN(C(c3ccccc3)c3ccccc3)CC2)on1)\c1ccccc1 10.1016/s0960-894x(02)00179-8
10994141 51698 0 None -6 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccnc2ccccc12 10.1021/jm020952a
CHEMBL152304 51698 0 None -6 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccnc2ccccc12 10.1021/jm020952a
164628178 193126 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 193126 0 None -46 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D4 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
71657942 97167 0 None -154 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 424 9 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386605 97167 0 None -154 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 424 9 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmc.2013.03.074
168268877 196749 0 None -134 12 Human 6.2 pKi = 6.2 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 196749 0 None -134 12 Human 6.2 pKi = 6.2 Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constantBinding affinity to D4 receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
44438204 100431 2 None -48 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 324 3 2 2 3.8 OC1(c2ccc(F)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246849 100431 2 None -48 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 324 3 2 2 3.8 OC1(c2ccc(F)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10786591 213508 0 None - 1 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)c(Cl)c1)CC3 10.1021/jm970170v
CHEMBL89913 213508 0 None - 1 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)c(Cl)c1)CC3 10.1021/jm970170v
3746693 209181 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm970111h
CHEMBL61080 209181 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm970111h
10786591 213508 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 389 3 0 4 4.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)c(Cl)c1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL89913 213508 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 389 3 0 4 4.7 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)c(Cl)c1)CC3 10.1016/j.ejmech.2020.113034
3746693 209181 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm0002432
CHEMBL61080 209181 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm0002432
155538028 179138 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 453 11 2 6 3.1 C=CCN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4475978 179138 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 453 11 2 6 3.1 C=CCN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
49782603 24261 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 385 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1257811 24261 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 385 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
3746693 209181 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm960072u
CHEMBL61080 209181 13 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
ChEMBL 385 4 1 2 5.8 Clc1ccc(CN2CCC(c3cc(-c4ccc(Cl)cc4)[nH]n3)CC2)cc1 10.1021/jm960072u
11187628 11644 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 363 6 0 4 4.3 COc1ccccc1SCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
CHEMBL104378 11644 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 363 6 0 4 4.3 COc1ccccc1SCC1CN(Cc2ccc(Cl)cc2)CCO1 10.1021/jm031111m
11164922 12150 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.0 COc1ccccc1OCC1CN(Cc2ccc(C(F)(F)F)cc2)CCO1 10.1021/jm031111m
CHEMBL107019 12150 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 381 6 0 4 4.0 COc1ccccc1OCC1CN(Cc2ccc(C(F)(F)F)cc2)CCO1 10.1021/jm031111m
9925730 213077 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 281 6 2 3 3.0 Cc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL87067 213077 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 281 6 2 3 3.0 Cc1nc2c(OCCNCc3ccccc3)cccc2[nH]1 10.1016/s0960-894x(99)00434-5
178078 127895 4 None -117 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 345 4 1 2 5.4 Oc1ccc(C2=CCC[C@@H](CN3CC=C(c4ccccc4)CC3)C2)cc1 10.1021/jm00026a007
CHEMBL357416 127895 4 None -117 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 345 4 1 2 5.4 Oc1ccc(C2=CCC[C@@H](CN3CC=C(c4ccccc4)CC3)C2)cc1 10.1021/jm00026a007
8704110 73375 9 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL185263 73375 9 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
44340302 16524 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL113471 16524 0 None 1 4 Human 6.2 pKi = 6.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
25139331 176707 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
CHEMBL444128 176707 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
137636298 162977 0 None -3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 245 1 3 4 0.6 O=c1ccc2c(N3CCNCC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
CHEMBL4064191 162977 0 None -3 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 245 1 3 4 0.6 O=c1ccc2c(N3CCNCC3)ccc(O)c2[nH]1 10.1016/j.bmc.2017.08.037
681 8247 72 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 8247 72 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 8247 72 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 8247 72 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 8247 72 None -2 38 Human 7.2 pKi = 7.2 Binding
Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
137643122 164814 0 None -17 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4085752 164814 0 None -17 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 467 8 2 10 2.6 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
10642106 45997 2 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2N1 10.1021/jm990277d
CHEMBL147011 45997 2 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement.
ChEMBL 357 3 1 4 3.0 O=C1COc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2N1 10.1021/jm990277d
49799715 21105 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 2 3 3.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1170879 21105 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 2 3 3.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200020 21105 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 2 3 3.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
44374648 126750 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 351 5 1 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
CHEMBL349843 126750 0 None -3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)Binding affinity was measured at cloned mammalian dopamine D4 receptor expressed in CHO-K1 cells (using [3H]- spiperone)
ChEMBL 351 5 1 4 3.3 CCCN[C@@H]1CCc2c(OS(=O)(=O)C(F)(F)F)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
176 7186 66 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -4 31 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
44336105 11708 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.5 CC(C)CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104713 11708 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 425 6 0 3 4.5 CC(C)CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
155195486 176466 0 None -14 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4437740 176466 0 None -14 3 Human 4.2 pKi = 4.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@@H]1C[C@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
46231847 207353 0 None -3162 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599116 207353 0 None -3162 4 Human 5.2 pKi = 5.2 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10544707 23073 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3oc(=O)ccc3c2)CC1 10.1021/jm990266k
CHEMBL122531 23073 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1ccccc1N1CCN(Cc2ccc3oc(=O)ccc3c2)CC1 10.1021/jm990266k
44426509 92518 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
CHEMBL229024 92518 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.096
242 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
34 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
60795 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
CHEMBL1112 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
DB01238 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
242 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
34 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
60795 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL1112 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
DB01238 7258 124 None -104 51 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
10357869 11656 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3cccc3-c3cnco3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL104453 11656 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3cccc3-c3cnco3)CC2)cc1 10.1016/s0960-894x(99)00540-5
44273920 80699 0 None 6 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 377 5 1 3 3.7 CC(C)(C)C(=O)NCCCCN1CCN2c3ccc(Cl)cc3CCC2C1 10.1016/0960-894X(96)00198-9
CHEMBL20204 80699 0 None 6 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 377 5 1 3 3.7 CC(C)(C)C(=O)NCCCCN1CCN2c3ccc(Cl)cc3CCC2C1 10.1016/0960-894X(96)00198-9
44273921 84137 0 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 6 1 3 3.8 CC1CN(CCCCNC(=O)C(C)(C)C)CCN1c1ccc(Cl)cc1 10.1016/0960-894X(96)00198-9
CHEMBL20854 84137 0 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 365 6 1 3 3.8 CC1CN(CCCCNC(=O)C(C)(C)C)CCN1c1ccc(Cl)cc1 10.1016/0960-894X(96)00198-9
4302960 107838 63 None -199 6 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine D4 receptorBinding affinity towards Dopamine D4 receptor
ChEMBL 485 10 1 5 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(C(C)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL294747 107838 63 None -199 6 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine D4 receptorBinding affinity towards Dopamine D4 receptor
ChEMBL 485 10 1 5 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(C(C)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
168268735 199548 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 4 0 3 2.8 O=C1CCc2ccccc2N1CCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5171721 199548 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 4 0 3 2.8 O=C1CCc2ccccc2N1CCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5221227 199548 0 None 16 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method
ChEMBL 335 4 0 3 2.8 O=C1CCc2ccccc2N1CCN1CCN(c2ccccc2)CC1 10.1021/acs.jmedchem.2c00840
CHEMBL5092243 222133 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(c3cccc(OC)c3)c3cccc(OC)c3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
10430816 175026 1 None 1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 395 8 1 4 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(C)c3C)CC2)c1 10.1021/jm020952a
CHEMBL433741 175026 1 None 1 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 395 8 1 4 3.6 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(C)c3C)CC2)c1 10.1021/jm020952a
49788868 24995 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 364 6 1 5 2.1 COc1cccc(C(=O)NCCN2CCN(c3ccc(C#N)cc3)CC2)c1 10.1021/jm100925m
CHEMBL1270120 24995 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 364 6 1 5 2.1 COc1cccc(C(=O)NCCN2CCN(c3ccc(C#N)cc3)CC2)c1 10.1021/jm100925m
44437896 159247 0 None -57 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 400 6 1 3 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL397103 159247 0 None -57 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cellsDisplacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells
ChEMBL 400 6 1 3 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)ccc1OC 10.1016/j.bmc.2007.07.017
10479822 89804 0 None -1778 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 469 7 2 4 4.7 N#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)[nH]c2c1 10.1021/jm0611152
CHEMBL218151 89804 0 None -1778 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 469 7 2 4 4.7 N#Cc1ccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)[nH]c2c1 10.1021/jm0611152
90389439 152477 2 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL3916231 152477 2 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
90389439 152477 2 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
CHEMBL3916231 152477 2 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 406 8 1 4 3.8 CC(O)CN1CCN(CCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.6b01373
52937871 67946 0 None -162 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 458 11 1 5 4.6 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(C=O)c2C1 10.1021/jm101639t
CHEMBL1765631 67946 0 None -162 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 minsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins
ChEMBL 458 11 1 5 4.6 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(C=O)c2C1 10.1021/jm101639t
12280575 17059 4 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL11615 17059 4 None -6 5 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 261 6 0 2 3.7 CCCN(CCC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
49798797 21128 0 None -10 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 2 3 3.7 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172208 21128 0 None -10 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 2 3 3.7 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200149 21128 0 None -10 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 433 3 2 3 3.7 OC1(c2ccc(I)cc2)CCN(Cc2c[nH]c3ncccc23)CC1 10.1016/j.bmc.2010.05.052
3038495 7495 37 None -91 18 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
7625 7495 37 None -91 18 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
CHEMBL25236 7495 37 None -91 18 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
72190766 99135 0 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
CHEMBL2430443 99135 0 None -12 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-spiperone from cloned human dopamine D4 receptorDisplacement of [3H]-spiperone from cloned human dopamine D4 receptor
ChEMBL 391 8 0 6 3.6 COc1ccccc1N1CCN(CCCCn2cc(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.08.047
44336175 114974 0 None -13 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 399 5 0 4 3.1 COc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL319650 114974 0 None -13 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 399 5 0 4 3.1 COc1cccc2c1CCN2C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
44339879 179061 0 None 4 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL447476 179061 0 None 4 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
10871118 213586 0 None 186 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccn4nccc34)CC2)cc1 10.1021/jm015522j
CHEMBL90374 213586 0 None 186 4 Human 7.2 pKi = 7.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccn4nccc34)CC2)cc1 10.1021/jm015522j
44335847 11833 0 None 36 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL105354 11833 0 None 36 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 363 4 0 3 3.1 Cc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
155536022 178882 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 467 11 2 6 3.5 C=C(C)CN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
CHEMBL4472580 178882 0 None 3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 467 11 2 6 3.5 C=C(C)CN(NC(=O)NCCCN1CCN(c2ccccc2OC)CC1)c1ccc(OC)cc1 10.1021/acs.jmedchem.9b01085
164614709 191988 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4857665 191988 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
57400556 76085 0 None -97 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928134 76085 0 None -97 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
56589560 77372 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
CHEMBL1949725 77372 0 None -14 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
164614709 191988 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4857665 191988 0 None -15 7 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 383 6 0 4 4.1 O=C1c2ccc(Cl)cc2CC1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
164621610 192970 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4872800 192970 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL5088070 221915 0 None -75 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cccc(N2CCN(CCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CC2)c1Cl 10.1021/acs.jmedchem.1c00611
24810004 23322 0 None -10 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 419 6 0 2 6.3 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL12375 23322 0 None -10 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 419 6 0 2 6.3 Fc1ccc(C(OC2CC3CCC(C2)N3Cc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
42626103 63027 0 None -1479 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627323 63027 0 None -1479 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
168274755 197421 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5181334 197421 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
168274755 197421 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
CHEMBL5181334 197421 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.bmcl.2022.128615
10039198 63123 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL163087 63123 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Dissociation constant of compound on one-site model Dopamine receptor D4.4Dissociation constant of compound on one-site model Dopamine receptor D4.4
ChEMBL 277 5 0 1 4.5 CCCN(CCC)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm991098z
11049209 214184 0 None -13182 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 486 6 1 5 4.4 Cn1ccc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL93923 214184 0 None -13182 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 486 6 1 5 4.4 Cn1ccc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
11658914 77015 1 None -30 3 Human 5.2 pKi = 5.2 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
CHEMBL194099 77015 1 None -30 3 Human 5.2 pKi = 5.2 Binding
Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandLow binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 255 5 0 3 3.0 CCCN(CCC)C1CCn2ncc(Cl)c2C1 10.1021/jm0503805
54456 169269 28 None -1 2 Human 5.2 pKi = 5.2 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 179 0 3 3 1.3 CC1NCCc2cc(O)c(O)cc21 10.1016/S0960-894X(97)00194-7
CHEMBL416732 169269 28 None -1 2 Human 5.2 pKi = 5.2 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 179 0 3 3 1.3 CC1NCCc2cc(O)c(O)cc21 10.1016/S0960-894X(97)00194-7
155568867 182933 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
CHEMBL4592753 182933 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 297 4 1 5 1.2 O=C(CN1CCN(c2ccccn2)CC1)Nc1cccnc1 10.1021/acs.jmedchem.9b00231
71658206 97182 0 None -42 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 416 8 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)nc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386620 97182 0 None -42 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 416 8 1 5 3.5 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Cl)nc2)CC1 10.1016/j.bmc.2013.03.074
11316709 175149 0 None 4 2 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
CHEMBL434532 175149 0 None 4 2 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
168274850 196934 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5173767 196934 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
168274755 197421 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
CHEMBL5181334 197421 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 403 5 0 4 4.8 Cn1cnc2cc(CN3CCC(OCc4cccc(C(F)(F)F)c4)CC3)ccc21 10.1016/j.ejmech.2022.114840
10761828 45449 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 372 4 1 5 4.4 Oc1nc2ccccc2n1C1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
CHEMBL146557 45449 0 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 372 4 1 5 4.4 Oc1nc2ccccc2n1C1CCN(Cc2ccn(-c3ccccc3)c2)CC1 10.1021/jm00025a013
168274850 196934 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5173767 196934 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.ejmech.2022.114840
168274850 196934 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5173767 196934 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 405 6 0 5 4.4 FC(F)(F)Oc1cccc(CO[C@H]2CCCN(Cc3cn4ccccc4n3)C2)c1 10.1016/j.bmcl.2022.128615
2993172 133945 4 None -32 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
CHEMBL365697 133945 4 None -32 3 Human 5.2 pKi = 5.2 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
9828632 106846 0 None -8 2 Human 7.2 pKi = 7.2 Binding
Affinity against D4 receptor was evaluatedAffinity against D4 receptor was evaluated
ChEMBL 535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/s0960-894x(98)00469-7
CHEMBL287198 106846 0 None -8 2 Human 7.2 pKi = 7.2 Binding
Affinity against D4 receptor was evaluatedAffinity against D4 receptor was evaluated
ChEMBL 535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/s0960-894x(98)00469-7
763343 98916 8 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 258 3 0 3 3.1 c1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
CHEMBL2420769 98916 8 None 25 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 258 3 0 3 3.1 c1ccc(N2CCN(Cc3cccs3)CC2)cc1 10.1016/j.bmcl.2013.07.033
10137747 126951 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1ccc(C)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
CHEMBL351612 126951 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 433 4 0 4 3.8 COc1ccc(C)cc1CN1CCN(C2CCc3cccc4c3N(C2=O)C(C)(C)C4)CC1 10.1016/s0960-894x(02)01056-9
164621610 192970 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4872800 192970 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 355 4 0 4 3.3 O=C1c2ccc(Cl)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
11676195 201927 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
CHEMBL550222 201927 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 423 8 1 6 3.4 CSc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm900690y
72737730 121304 0 None 42 3 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335554 121304 0 None 42 3 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 365 6 0 3 4.4 FC(F)(F)Oc1ccc(CN2CCO[C@H](CCc3ccccc3)C2)cc1 10.1021/ml500267c
155535272 178810 0 None -177 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 280 5 0 2 3.8 CCCCN1CCN(c2cccc(CC)c2Cl)CC1 10.1021/acs.jmedchem.6b00860
CHEMBL4471669 178810 0 None -177 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 280 5 0 2 3.8 CCCCN1CCN(c2cccc(CC)c2Cl)CC1 10.1021/acs.jmedchem.6b00860
60165535 82125 0 None -12 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 322 5 0 3 4.7 c1ccc2c(c1)CCN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
CHEMBL2037522 82125 0 None -12 6 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 322 5 0 3 4.7 c1ccc2c(c1)CCN(CCCCc1nc3ccccc3s1)C2 10.1016/j.ejmech.2012.03.042
11428005 11829 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2cccc(Cl)c2)CCO1 10.1021/jm031111m
CHEMBL105312 11829 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccccc1OCC1CN(Cc2cccc(Cl)c2)CCO1 10.1021/jm031111m
44304643 210054 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 8 0 5 5.1 COc1ccc(Br)cc1-c1nc(CN(C)C[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64668 210054 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 469 8 0 5 5.1 COc1ccc(Br)cc1-c1nc(CN(C)C[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
11028157 209500 0 None -8 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1021/jm020952a
CHEMBL61789 209500 0 None -8 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 563 8 1 4 6.3 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1021/jm020952a
30982708 17454 5 None -134 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 384 3 2 2 4.4 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1170683 17454 5 None -134 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 384 3 2 2 4.4 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmc.2010.05.052
71658203 97179 0 None -57 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 483 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc3c2-c2ccccc2C3=O)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386617 97179 0 None -57 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 483 8 1 5 4.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2cccc3c2-c2ccccc2C3=O)CC1 10.1016/j.bmc.2013.03.074
11247757 140357 0 None 10 2 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
CHEMBL371200 140357 0 None 10 2 Rat 6.2 pKi = 6.2 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1CC[C@H]1CN(CCCCNC(=O)c3ccc4ccccc4c3)CCN21 10.1021/jm049031l
44431465 157516 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL395631 157516 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 422 4 1 2 5.0 O=C(NC1CCN(Cc2cccc(Br)c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
137645574 164582 0 None -70 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4083239 164582 0 None -70 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
45271691 202332 0 None 46 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 3 0 5 3.6 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL554692 202332 0 None 46 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 369 3 0 5 3.6 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
45272580 203235 0 None 13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cnc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL563109 203235 0 None 13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cnc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
145993700 174109 0 None -75 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 370 7 3 5 2.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(O)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4294279 174109 0 None -75 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 370 7 3 5 2.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(O)cc1)CC2 10.1021/acsmedchemlett.8b00229
56833379 75109 0 None -54 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1155 37 2 18 8.6 COc1cc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL1916550 75109 0 None -54 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 1155 37 2 18 8.6 COc1cc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL5089932 222012 0 None -25 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NC[C@@H]2CCCN2CCCCNCCC(C(=O)N(C)C)(c2ccccc2)c2ccccc2)c1O 10.1021/acs.jmedchem.1c00611
46227273 206590 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 3 0 2 3.8 COc1ccc2c(c1)CCN(C)C2Cc1ccccc1C 10.1016/j.bmc.2009.08.028
CHEMBL594127 206590 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]spiperone from human dopamine D4 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 3 0 2 3.8 COc1ccc2c(c1)CCN(C)C2Cc1ccccc1C 10.1016/j.bmc.2009.08.028
155195487 180055 0 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
CHEMBL4525362 180055 0 None -14 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1CC1CC1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.9b00702
49799709 21178 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3cccc(OCCF)c23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1173711 21178 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3cccc(OCCF)c23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200302 21178 0 None -24 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 446 6 2 3 4.8 OC1(c2ccc(Br)cc2)CCN(Cc2c[nH]c3cccc(OCCF)c23)CC1 10.1016/j.bmc.2010.05.052
44361021 125564 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm025558r
CHEMBL342060 125564 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm025558r
44335971 12089 0 None 18 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 CC(c1ccc(Cl)cc1)N1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106751 12089 0 None 18 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 CC(c1ccc(Cl)cc1)N1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
10740969 105862 0 None 3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.4 COc1ccccc1N1CCN(CCC(=O)NC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL28063 105862 0 None 3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 423 7 1 5 3.4 COc1ccccc1N1CCN(CCC(=O)NC2CCCc3c(OC)cccc32)CC1 10.1016/S0960-894X(97)00218-7
11849267 86647 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL212292 86647 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 372 6 0 5 3.7 CO/N=C(\CCN1CCN(c2ccccn2)CC1C)c1ccc(Cl)cc1 10.1021/jm060279f
127052488 147577 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
CHEMBL3818799 147577 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
11133602 37548 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
CHEMBL139600 37548 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm0611152
44361021 125564 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm0611152
CHEMBL342060 125564 0 None -23 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm0611152
45361874 176800 2 None 48 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4442548 176800 2 None 48 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 324 5 1 4 2.4 CCc1cccc(NC(=O)CN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
25139481 191619 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1021/jm800895v
CHEMBL485227 191619 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1021/jm800895v
154706590 183088 1 None -36 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4590839 183088 1 None -36 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4595264 183088 1 None -36 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
127049061 147545 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818398 147545 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL5081136 221504 0 None -309 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None CCc1cc(Cl)c(OC)c(C(=O)NC[C@@H]2C[C@@H](OCCCCNCCC(C(=O)N(C)C)(c3ccccc3)c3ccccc3)CN2)c1O 10.1021/acs.jmedchem.1c00611
155516042 183072 0 None -446 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4443039 183072 0 None -446 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595150 183072 0 None -446 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
154703875 183227 1 None -52 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4586582 183227 1 None -52 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596341 183227 1 None -52 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
10827222 13757 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL108463 13757 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human dopamine receptor D4 was determinedBinding affinity towards human dopamine receptor D4 was determined
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1016/j.bmcl.2005.02.012
127049061 147545 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3818398 147545 0 None -4 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 440 6 1 5 5.3 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3s2)CC1 10.1016/j.bmc.2016.06.011
44438231 100384 3 None -4 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 2 3 4.4 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246642 100384 3 None -4 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 375 3 2 3 4.4 OC1(c2ccc(Cl)c(Cl)c2)CCN(Cc2n[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
10927750 14150 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
CHEMBL108637 14150 0 None 1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm010146o
44438208 100145 2 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 336 4 2 3 3.7 COc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
CHEMBL245614 100145 2 None -3 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 336 4 2 3 3.7 COc1ccc(C2(O)CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.10.076
11133602 37548 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL139600 37548 0 None -3 5 Human 7.2 pKi = 7.2 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
10713620 46167 1 None -19 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 361 4 2 3 5.1 Oc1ccc(C2=CCN(C[C@@H]3CCC=C(c4ccc(O)cc4)C3)CC2)cc1 10.1021/jm00026a007
CHEMBL147159 46167 1 None -19 3 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 361 4 2 3 5.1 Oc1ccc(C2=CCN(C[C@@H]3CCC=C(c4ccc(O)cc4)C3)CC2)cc1 10.1021/jm00026a007
127052488 147577 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
CHEMBL3818799 147577 0 None -2 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 477 8 0 4 6.3 Fc1ccc(C(c2ccc(F)cc2)N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2016.06.011
57390118 76077 0 None -77 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928126 76077 0 None -77 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
22100970 109602 4 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc(CN2CC=C(c3nc4ccccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL305481 109602 4 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 323 3 1 2 4.5 Clc1ccc(CN2CC=C(c3nc4ccccc4[nH]3)CC2)cc1 10.1016/S0960-894X(97)00402-2
10073022 92833 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 461 9 0 2 7.1 Fc1ccc(C(O[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL2308105 92833 0 None -4 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 461 9 0 2 7.1 Fc1ccc(C(O[C@@H]2C[C@@H]3CC[C@H](C2)N3CCCCc2ccccc2)c2ccc(F)cc2)cc1 10.1021/jm010146o
72545008 99898 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443001 99898 0 None 1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
10960333 213763 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 398 5 0 6 3.5 CCOC(=O)c1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
CHEMBL91362 213763 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperoneBinding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone
ChEMBL 398 5 0 6 3.5 CCOC(=O)c1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
10827222 13757 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
CHEMBL108463 13757 1 None -61 5 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligandBinding affinity against human Dopamine receptor D4 in CHO-K1 cells using [3H]spiperone as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
44275820 20739 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 7 0 4 4.8 Cc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1196753 20739 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 7 0 4 4.8 Cc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL558036 20739 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 375 7 0 4 4.8 Cc1ccccc1N1CCN(CCCCc2cc(-c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
44123782 196379 0 None -6 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
CHEMBL514747 196379 0 None -6 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 10.1016/j.bmc.2008.12.054
71456889 88599 0 None -36 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2cccc3ccccc23)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
CHEMBL2164348 88599 0 None -36 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 466 7 0 5 4.7 COc1ccccc1N1CCN(CCN(C(=O)c2cccc3ccccc23)c2ccccn2)CC1 10.1016/j.bmcl.2012.05.119
44431476 94352 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
CHEMBL233578 94352 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1ccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)cc1 10.1016/j.bmcl.2006.12.106
25139477 191024 0 None -15 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
CHEMBL483593 191024 0 None -15 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
44436618 154701 0 None -45 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1ccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL393365 154701 0 None -45 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 443 8 1 3 4.7 C#Cc1ccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
130442572 178687 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 178687 0 None -147 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442480 182049 0 None -85 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 182049 0 None -85 24 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
2812 11551 101 None -39 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 11551 101 None -39 34 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
44340333 16434 0 None 19 4 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL112833 16434 0 None 19 4 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
21462980 53909 0 None 23 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1ccc2c(c1)CCN(Cc1c[nH]c3ncccc13)C2 10.1016/s0960-894x(99)00025-6
CHEMBL154286 53909 0 None 23 3 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cellsAbility to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells
ChEMBL 263 2 1 2 3.1 c1ccc2c(c1)CCN(Cc1c[nH]c3ncccc13)C2 10.1016/s0960-894x(99)00025-6
2389 10104 118 None -22 66 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
5073 10104 118 None -22 66 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
96 10104 118 None -22 66 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
CHEMBL85 10104 118 None -22 66 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
DB00734 10104 118 None -22 66 Human 8.2 pKi = 8.2 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm00004a016
9861459 170897 0 None -17 4 Human 8.2 pKi = 8.2 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
CHEMBL420986 170897 0 None -17 4 Human 8.2 pKi = 8.2 Binding
Affinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperoneAffinity for the Human Dopamine receptor D4 was determined using membranes from CHO cells labeled with [3H]spiperone
ChEMBL 309 4 3 4 2.8 Oc1nc2c3c(ccc2[nH]1)CC[C@H](CNCc1ccccc1)O3 10.1016/s0960-894x(01)00778-8
6469918 86666 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1016/j.ejmech.2019.111569
CHEMBL212370 86666 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1016/j.ejmech.2019.111569
10646834 113941 0 None 33 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL316317 113941 0 None 33 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 441 7 2 4 4.1 COc1cc(NC(=O)C2CCC2)c(Cl)cc1C(=O)N[C@@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
44336099 117465 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL326010 117465 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 417 4 0 3 4.1 C[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2cc(Cl)cc(Cl)c2)CC1 10.1016/s0960-894x(02)00656-x
44336051 118083 0 None 16 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
CHEMBL326670 118083 0 None 16 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 4.0 C[C@@H]1c2ccccc2N(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)[C@@H]1C 10.1016/s0960-894x(02)00655-8
44335798 11617 0 None 213 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104256 11617 0 None 213 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 363 4 0 3 3.1 Cc1ccccc1CN1CCN(CC(=O)N2c3ccccc3CC2C)CC1 10.1016/s0960-894x(02)00655-8
44335924 11687 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 367 4 0 3 2.9 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104614 11687 0 None 125 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 367 4 0 3 2.9 CC1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(02)00655-8
44335886 11712 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104719 11712 0 None 7 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 366 4 0 2 4.4 CC1Cc2ccccc2N1C(=O)CC1CCN(Cc2cccc(F)c2)CC1 10.1016/s0960-894x(02)00655-8
44335991 11728 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 5 0 4 2.8 O=S1(=O)Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104800 11728 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 405 5 0 4 2.8 O=S1(=O)Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
1353 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
3559 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
86 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
CHEMBL54 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
DB00502 8692 93 None -3 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00025a013
44405522 78704 0 None 251 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 406 5 1 5 4.1 O=C(N[C@H]1CCN(Cc2ccc3c(c2)OCO3)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL197225 78704 0 None 251 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 406 5 1 5 4.1 O=C(N[C@H]1CCN(Cc2ccc3c(c2)OCO3)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
6469918 86666 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 86666 13 None 169 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membraneDisplacement of [3H]spiperone from human dopamine receptor D4.4 in CHO cell membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
11338828 11807 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL105181 11807 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1cc(Cl)ccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
9820680 212983 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 369 6 2 3 4.4 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
CHEMBL86504 212983 0 None -2 4 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 369 6 2 3 4.4 FC(F)(F)c1nc2c(OCCNCc3ccccc3)cc(Cl)cc2[nH]1 10.1016/s0960-894x(99)00434-5
681 8247 72 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
940 8247 72 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
947 8247 72 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
CHEMBL59 8247 72 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
DB00988 8247 72 None -2 38 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401384w
71151588 125036 0 None -70 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
CHEMBL3409256 125036 0 None -70 10 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]methylspiperone from human dopamine D4 receptor expressed in CHO cells
ChEMBL 518 9 1 7 3.6 NC(=O)c1ccccc1OCCCN1CCN(c2cccc3c2ccn3S(=O)(=O)c2ccccc2)CC1 10.1016/j.ejmech.2014.12.045
25071385 165936 0 None -3 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 165936 0 None -3 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
133079 10410 42 None -1 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm960084f
980 10410 42 None -1 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm960084f
CHEMBL69759 10410 42 None -1 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.Binding affinity of [3H]spiperone towards Dopamine receptor D4 expressed in cultured cells or from rat whole brain.
ChEMBL 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 10.1021/jm960084f
2563 10523 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
55 10523 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
91273 10523 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
CHEMBL274047 10523 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
DB12833 10523 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1016/s0960-894x(01)00167-6
53361302 70624 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803049 70624 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
53361302 70624 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1803049 70624 0 None 4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
1353 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
3559 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
86 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
CHEMBL54 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
DB00502 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049612a
1353 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
3559 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
86 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
CHEMBL54 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
DB00502 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant dopamine receptor D4.2Binding affinity for human recombinant dopamine receptor D4.2
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
1353 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
3559 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
86 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
CHEMBL54 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
DB00502 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm960637m
10905940 51976 0 None 16 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 421 7 1 4 3.9 COc1cccc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL152576 51976 0 None 16 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 421 7 1 4 3.9 COc1cccc(C(=O)NCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
56926586 75784 0 None 316 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 344 3 1 5 2.6 Oc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
CHEMBL1923415 75784 0 None 316 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 344 3 1 5 2.6 Oc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
44339953 116477 0 None 3 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
CHEMBL322802 116477 0 None 3 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
72164181 98922 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
CHEMBL2420774 98922 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 274 3 1 4 2.8 Oc1ccccc1N1CCN(Cc2cccs2)CC1 10.1016/j.bmcl.2013.07.033
127027905 146234 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
CHEMBL3794079 146234 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 327 5 0 3 4.3 Cc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1C 10.1016/j.bmcl.2016.03.102
3069135 76939 3 None 3 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 3 3.4 Fc1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940412 76939 3 None 3 6 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 314 6 0 3 3.4 Fc1ccc(OCCCN2CCN(c3ccccc3)CC2)cc1 10.1016/j.bmc.2011.12.019
10687362 113384 0 None 288 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 323 2 0 3 3.8 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
CHEMBL314285 113384 0 None 288 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 323 2 0 3 3.8 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1021/jm970170v
10570898 213274 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 366 4 0 6 3.3 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc([N+](=O)[O-])cc1)CC3 10.1021/jm970170v
CHEMBL88296 213274 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 366 4 0 6 3.3 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc([N+](=O)[O-])cc1)CC3 10.1021/jm970170v
10687362 113384 0 None 288 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 323 2 0 3 3.8 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL314285 113384 0 None 288 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 323 2 0 3 3.8 Cc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(F)cc1)CC3 10.1016/j.ejmech.2020.113034
10833953 37898 0 None 1445 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140006 37898 0 None 1445 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cc2c1 10.1021/jm0009989
11811640 172045 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 408 8 1 6 3.2 COc1cccc(C(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm020952a
CHEMBL423040 172045 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 408 8 1 6 3.2 COc1cccc(C(=O)NCCCCN2CCN(c3noc4ccccc34)CC2)c1 10.1021/jm020952a
44395741 188360 0 None 1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL476935 188360 0 None 1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL558392 188360 0 None 1 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
44372009 55613 0 None 109 4 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 402 4 0 4 5.0 Clc1ccc(N2CCN(Cc3cnn4c(-c5ccccc5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL155913 55613 0 None 109 4 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 402 4 0 4 5.0 Clc1ccc(N2CCN(Cc3cnn4c(-c5ccccc5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
10593191 195887 1 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
CHEMBL51023 195887 1 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1021/jm970021c
10593191 195887 1 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
CHEMBL51023 195887 1 None 33 3 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 339 5 1 4 2.5 COc1ccccc1N1CCN(CNC(=O)c2ccc(C)cc2)CC1 10.1016/j.bmcl.2005.02.012
2402 10143 62 None -1 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
5095 10143 62 None -1 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
7295 10143 62 None -1 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
CHEMBL589 10143 62 None -1 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
DB00268 10143 62 None -1 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D4 receptorBinding affinity to human dopamine D4 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
9798466 141056 1 None 1 6 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1021/jm0002432
CHEMBL37170 141056 1 None 1 6 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1021/jm0002432
57401819 76935 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940408 76935 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57401819 76935 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940408 76935 0 None 10 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
137657115 166534 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 166534 0 None -3 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
9798466 141056 1 None 1 6 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL37170 141056 1 None 1 6 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
10568805 175946 0 None 74 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 4 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(CCc1ccccc1)CC3 10.1021/jm970170v
CHEMBL440506 175946 0 None 74 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 335 4 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(CCc1ccccc1)CC3 10.1021/jm970170v
10568805 175946 0 None 74 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 335 4 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(CCc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL440506 175946 0 None 74 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 335 4 0 4 3.4 COc1ccc2c3c(c(=O)oc2c1)CN(CCc1ccccc1)CC3 10.1016/j.ejmech.2020.113034
164620912 192514 0 None -1 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 1 4 2.6 OC1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
CHEMBL4866053 192514 0 None -1 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor incubated for 1 hr by liquid scintillation counting method
ChEMBL 341 4 1 4 2.6 OC1c2ccc(F)cc2CC1CCN1CCN(c2ccccn2)CC1 10.1016/j.ejmech.2021.113243
137640371 163593 0 None -5 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071185 163593 0 None -5 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
1353 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
3559 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
86 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
CHEMBL54 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
DB00502 8692 93 None -3 85 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
44273908 83491 0 None 100 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 363 5 1 3 3.5 CC1(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
CHEMBL20655 83491 0 None 100 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 363 5 1 3 3.5 CC1(C(=O)NCCN2CCN(c3ccc(Cl)cc3)CC2)CCCCC1 10.1016/0960-894X(96)00198-9
44273887 83826 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 7 1 3 3.4 CCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL20725 83826 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 7 1 3 3.4 CCCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
10359736 106290 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
CHEMBL283353 106290 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/0960-894X(96)00198-9
44394675 173151 0 None 53 2 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL427522 173151 0 None 53 2 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 384 6 1 3 4.2 O=Cc1ccc(-c2ccc(C(=O)NC3CCN(Cc4ccccc4)C3)cc2)cc1 10.1016/j.bmcl.2004.07.045
135398737 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
38 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
722 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
CHEMBL42 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
DB00363 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960637m
57391897 76084 0 None -7 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928133 76084 0 None -7 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
45270021 201943 0 None 60 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 335 3 0 5 3.0 Cc1cc2nc(C)c(CN3CCN(c4ccccc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL550392 201943 0 None 60 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 335 3 0 5 3.0 Cc1cc2nc(C)c(CN3CCN(c4ccccc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
11382447 116443 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccc(Cl)cc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
CHEMBL322519 116443 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1ccc(Cl)cc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
60149678 121295 0 None 229 2 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
CHEMBL3335537 121295 0 None 229 2 Human 7.2 pKi = 7.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 321 5 1 3 3.4 c1ccc(CC[C@@H]2CN(Cc3nc4ccccc4[nH]3)CCO2)cc1 10.1021/ml500267c
57267 8374 14 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
966 8374 14 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
CHEMBL8946 8374 14 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
DB15492 8374 14 None -416 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay
ChEMBL 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 10.1021/acs.jmedchem.6b01373
9865858 170084 0 None -44 8 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against Dopamine receptor D4The compound was tested for binding affinity against Dopamine receptor D4
ChEMBL 402 6 1 5 4.0 COc1ccccc1N1CCC(CNCC2COc3ccc(Cl)cc3O2)CC1 10.1021/jm9910122
CHEMBL418854 170084 0 None -44 8 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against Dopamine receptor D4The compound was tested for binding affinity against Dopamine receptor D4
ChEMBL 402 6 1 5 4.0 COc1ccccc1N1CCC(CNCC2COc3ccc(Cl)cc3O2)CC1 10.1021/jm9910122
49798879 17383 6 None -275 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
CHEMBL1170096 17383 6 None -275 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1ccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c2c1 10.1016/j.bmc.2010.05.052
44319369 212598 0 None 2 4 Human 6.2 pKi = 6.2 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
CHEMBL83306 212598 0 None 2 4 Human 6.2 pKi = 6.2 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
44380716 65861 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL169631 65861 0 None 1 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44324980 214200 0 None -1318 3 Human 5.2 pKi = 5.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 249 2 1 4 1.9 CCCN1COC[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm960345l
CHEMBL94015 214200 0 None -1318 3 Human 5.2 pKi = 5.2 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 249 2 1 4 1.9 CCCN1COC[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm960345l
10310103 114089 0 None -1778 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL317333 114089 0 None -1778 9 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
9865920 114310 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(Cl)cc21 10.1016/s0960-894x(02)00655-8
CHEMBL318739 114310 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccc(Cl)cc21 10.1016/s0960-894x(02)00655-8
9887092 109451 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 5 0 3 4.1 CCN1C(=O)C(CC)(N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(00)00421-2
CHEMBL304584 109451 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.Binding affinity at human Dopamine receptor D4 by [3H]- YM 09151 displacement.
ChEMBL 397 5 0 3 4.1 CCN1C(=O)C(CC)(N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(00)00421-2
71658338 97185 0 None -97 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 410 9 2 5 3.5 CNc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
CHEMBL2386623 97185 0 None -97 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 410 9 2 5 3.5 CNc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
10569690 213852 11 None 3 3 Human 7.2 pKi = 7.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1nc(O)n(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1021/jm991029k
CHEMBL91821 213852 11 None 3 3 Human 7.2 pKi = 7.2 Binding
Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell linesAffinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines
ChEMBL 347 4 1 4 4.4 Cc1nc(O)n(C2CCN(Cc3ccccc3)CC2)c1-c1ccccc1 10.1021/jm991029k
73346042 98609 5 None -707 17 Human 7.2 pKi = 7.2 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 98609 5 None -707 17 Human 7.2 pKi = 7.2 Binding
Binding affinity to dopamine 4 receptor (unknown origin)Binding affinity to dopamine 4 receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
135398737 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
38 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
722 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
CHEMBL42 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
DB00363 7745 93 None -13 90 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00025a013
56649648 74630 0 None -213 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910139 74630 0 None -213 8 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 474 8 0 5 3.0 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52CF)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
44426499 148843 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
CHEMBL387951 148843 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 372 6 1 2 4.7 O=C(NC1CCN(CCCc2ccccc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.096
11451703 145796 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
CHEMBL378576 145796 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 376 6 0 5 3.4 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccc(F)c(Cl)c1 10.1021/jm060279f
12050195 210063 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 6 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64696 210063 0 None 1 4 Human 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
ChEMBL 441 6 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
130431287 177996 0 None -223 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 469 9 1 5 5.0 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
CHEMBL4459533 177996 0 None -223 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 469 9 1 5 5.0 CCc1cc(Cl)c(OC)c(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/acs.jmedchem.6b00860
44315403 212250 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
CHEMBL80469 212250 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 327 3 1 4 2.9 Clc1ccccc1N1CCN(Cc2nc3ccc[nH]c-3n2)CC1 10.1021/jm0305669
44278456 106662 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 373 7 0 2 5.8 CC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
CHEMBL28596 106662 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 373 7 0 2 5.8 CC(COc1cccc2ccccc12)CN1CCC(Cc2ccccc2)CC1 10.1016/S0960-894X(97)00233-3
122205438 144178 0 None -47 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL3753266 144178 0 None -47 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
11121216 36912 0 None -36 14 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL138989 36912 0 None -36 14 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
128054 211920 10 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1ccsc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL7806 211920 10 None -39 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 315 6 1 3 4.3 CCCN(CCc1ccsc1)C1CCc2c(O)cccc2C1 10.1021/jm960345l
127032085 146166 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
CHEMBL3793266 146166 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 363 5 0 5 3.3 FC1(F)Oc2ccc(CN3CCO[C@H](COc4ccccc4)C3)cc2O1 10.1016/j.bmcl.2016.03.102
10247720 19826 1 None 2 5 Human 7.1 pKi = 7.1 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 19826 1 None 2 5 Human 7.1 pKi = 7.1 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 19826 1 None 2 5 Human 7.1 pKi = 7.1 Binding
In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cellsIn vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
135398737 7745 93 None -13 90 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
38 7745 93 None -13 90 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
722 7745 93 None -13 90 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
CHEMBL42 7745 93 None -13 90 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
DB00363 7745 93 None -13 90 Human 7.1 pKi = 7.1 Binding
Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptorPotency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/S0960-894X(97)00194-7
49798853 21081 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 363 3 1 4 4.4 O=c1[nH]c2ccccc2n1C1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1169895 21081 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 363 3 1 4 4.4 O=c1[nH]c2ccccc2n1C1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1199932 21081 0 None -1 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 363 3 1 4 4.4 O=c1[nH]c2ccccc2n1C1CCN(Cc2csc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
10254390 78463 0 None -5623 7 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm020952a
CHEMBL196476 78463 0 None -5623 7 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 475 8 1 5 5.1 COc1cccc2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)oc12 10.1021/jm020952a
10961938 126317 0 None -1202 7 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm020952a
CHEMBL345820 126317 0 None -1202 7 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm020952a
145993377 173747 0 None -269 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 430 8 2 4 4.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(-c3ccccc3)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4287471 173747 0 None -269 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 430 8 2 4 4.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(-c3ccccc3)cc1)CC2 10.1021/acsmedchemlett.8b00229
11071135 214787 0 None -3311 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
CHEMBL97333 214787 0 None -3311 8 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
137646281 164585 0 None -1659 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 164585 0 None -1659 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
44336003 12395 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 389 4 0 3 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCC2CCCCC21 10.1016/s0960-894x(02)00655-8
CHEMBL107755 12395 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 389 4 0 3 3.6 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCCC2CCCCC21 10.1016/s0960-894x(02)00655-8
44336100 116553 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.5 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2[C@H]2CCCC[C@H]21 10.1016/s0960-894x(02)00655-8
CHEMBL323213 116553 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 423 4 0 3 4.5 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1c2ccccc2[C@H]2CCCC[C@H]21 10.1016/s0960-894x(02)00655-8
30743524 11667 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 3 3.4 O=C(CCN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL104498 11667 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 5 0 3 3.4 O=C(CCN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2ccccc21 10.1016/s0960-894x(02)00655-8
44336031 11984 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.6 CC1Cc2ccccc2N1C(=O)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106170 11984 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 382 4 0 2 4.6 CC1Cc2ccccc2N1C(=O)CN1CCC(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
71657946 97171 0 None -398 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 407 9 1 4 4.1 C=Cc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
CHEMBL2386609 97171 0 None -398 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 407 9 1 4 4.1 C=Cc1ccc(C(=O)NCCCCN2CCCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2013.03.074
10559624 33161 2 None -512 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 1 1 2 1.8 CN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
CHEMBL135932 33161 2 None -512 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 191 1 1 2 1.8 CN(C)C1CCc2ccc(O)cc2C1 10.1021/jm960345l
10494689 18339 1 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL1180589 18339 1 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL134343 18339 1 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@@H](CNCc1ccccc1)O2 10.1021/jm9703653
10495881 115965 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4cccnc4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL321513 115965 0 None 3 3 Human 7.1 pKi = 7.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4cccnc4)CC3)c[nH]2)cc1 10.1021/jm960637m
30616772 11560 0 None 112 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 371 5 0 5 3.1 O=c1oc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL104063 11560 0 None 112 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 371 5 0 5 3.1 O=c1oc2ccccc2n1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
127028183 146094 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
CHEMBL3792532 146094 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 366 6 0 5 3.2 COc1ccc(CN2CCO[C@H](COc3cccc(F)n3)C2)cc1Cl 10.1016/j.bmcl.2016.03.102
9886609 172108 0 None -6 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligandIn vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligand
ChEMBL 388 5 1 3 5.0 c1ccc(N2CCN(CC[C@H]3CC[C@H](c4c[nH]c5ccccc54)CC3)CC2)nc1 10.1021/jm960597m
CHEMBL423499 172108 0 None -6 3 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligandIn vitro binding affinity towards human recombinant Dopamine receptor D4 expressed in CHO-K1 cells was determined using [3H]spiperone as radioligand
ChEMBL 388 5 1 3 5.0 c1ccc(N2CCN(CC[C@H]3CC[C@H](c4c[nH]c5ccccc54)CC3)CC2)nc1 10.1021/jm960597m
127027238 146189 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3793709 146189 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 318 5 0 4 3.0 Clc1ccc(CN2CCO[C@H](COc3ccccn3)C2)cc1 10.1016/j.bmcl.2016.03.102
44264641 211581 1 None 4 3 Human 5.1 pKi = 5.1 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 230 2 0 4 1.1 CN1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7505 211581 1 None 4 3 Human 5.1 pKi = 5.1 Binding
Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4
ChEMBL 230 2 0 4 1.1 CN1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
12581219 32034 2 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 0 2 2.1 COc1cccc2c1CCC(N(C)C)C2 10.1021/jm960345l
CHEMBL134866 32034 2 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 2 0 2 2.1 COc1cccc2c1CCC(N(C)C)C2 10.1021/jm960345l
137645416 164706 0 None - 1 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000587a DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000587a DRD4
ChEMBL 302 3 1 5 1.5 CCNC(=O)c1cc2c(N3CCOC[C@@H]3C)ccnc2n1C 10.6019/CHEMBL5212743
CHEMBL4084419 164706 0 None - 1 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000587a DRD4Selectivity interaction (GPCR panel (PDSP screen)) EUB0000587a DRD4
ChEMBL 302 3 1 5 1.5 CCNC(=O)c1cc2c(N3CCOC[C@@H]3C)ccnc2n1C 10.6019/CHEMBL5212743
10567839 213812 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1021/jm970170v
CHEMBL91585 213812 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1021/jm970170v
44278853 112574 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 405 8 1 4 4.5 COc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
CHEMBL31269 112574 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.Binding affinity against human cloned D4 receptor transfected in CHO-K1 cells by [3H]- spiperone displacement.
ChEMBL 405 8 1 4 4.5 COc1ccc(CC2CCN(CC(O)COc3cccc4ccccc34)CC2)cc1 10.1016/S0960-894X(97)00233-3
10567839 213812 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL91585 213812 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 322 3 0 5 2.8 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccncc1)CC3 10.1016/j.ejmech.2020.113034
10636896 25656 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
CHEMBL128313 25656 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperoneBinding affinity to recombinant human dopamine receptor D4 expressed in CHO cells by displacement of [3H]spiperone
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1021/jm970422s
10688157 22353 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)c1 10.1021/jm990266k
CHEMBL122116 22353 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 334 3 0 4 3.4 Cc1cccc(N2CCN(Cc3ccc4oc(=O)ccc4c3)CC2)c1 10.1021/jm990266k
10636896 25656 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
CHEMBL128313 25656 1 None -3 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determinedBinding affinity to displace [3H]spiperone from cloned human dopamine receptor D4 was determined
ChEMBL 285 9 1 3 3.4 Cc1ccccc1OCCNCCCOc1ccccc1 10.1016/j.bmcl.2005.02.012
118719925 122557 0 None 7 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/acs.jmedchem.8b00265
CHEMBL3354072 122557 0 None 7 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 330 7 1 3 2.8 O=C1CCc2ccccc2N1CCCN1CCC(CCCO)CC1 10.1021/acs.jmedchem.8b00265
71658077 97178 0 None -56 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 425 10 2 5 3.0 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCO)cc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386616 97178 0 None -56 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 425 10 2 5 3.0 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(CCO)cc2)CC1 10.1016/j.bmc.2013.03.074
9884771 23370 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 350 4 0 5 3.1 COc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
CHEMBL124050 23370 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 350 4 0 5 3.1 COc1ccc(N2CCN(Cc3ccc4ccc(=O)oc4c3)CC2)cc1 10.1021/jm990266k
137657427 166338 0 None -67 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 476 7 3 6 3.5 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4102628 166338 0 None -67 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 476 7 3 6 3.5 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
11570471 148695 0 None -21 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 568 12 1 7 4.4 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
CHEMBL386986 148695 0 None -21 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 568 12 1 7 4.4 CCCc1c(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)nnn1Cc1ccccc1Br 10.1021/jm0611152
CHEMBL4579981 220797 11 None - 1 Human 5.1 pKi = 5.1 Binding
Affinity Biochemical interaction (Radioligand binding assay) EUB0000338a DRD4Affinity Biochemical interaction (Radioligand binding assay) EUB0000338a DRD4
ChEMBL None None None Cc1ccc2[nH]c(CNCCCc3ccncc3)cc(=O)c2c1 10.6019/CHEMBL5210307
11092112 214407 0 None -13489 9 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL95175 214407 0 None -13489 9 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
46231924 207357 0 None -1737 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL599134 207357 0 None -1737 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
118719807 122512 0 None -81 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 434 9 0 7 3.5 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(N(C)C)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353910 122512 0 None -81 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 434 9 0 7 3.5 COc1ccccc1N1CCN(CCCCc2cn(-c3ccc(N(C)C)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
44403220 78701 0 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(F)n2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL197214 78701 0 None -3 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(F)n2)CC1 10.1016/j.bmcl.2005.07.037
10375676 121981 37 None -99 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2c(O)cccc2C1 10.1021/jm960345l
CHEMBL334472 121981 37 None -99 3 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 205 3 2 2 2.2 CCCNC1CCc2c(O)cccc2C1 10.1021/jm960345l
56597938 10712 3 None -204 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
7651 10712 3 None -204 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL2165126 10712 3 None -204 9 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
122189394 130027 0 None -245 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 7 0 7 4.4 Clc1cccc(N2CCN(CCCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613880 130027 0 None -245 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 7 0 7 4.4 Clc1cccc(N2CCN(CCCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
22727361 20029 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL1191469 20029 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
CHEMBL542573 20029 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)c(OC)c1 10.1016/s0960-894x(02)00179-8
155530763 178348 0 None 9 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4464861 178348 0 None 9 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting methodDisplacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method
ChEMBL 323 5 1 3 3.6 Cc1cccc(NC(=O)CCN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
137655594 165419 0 None -18 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 287 3 2 4 1.8 CCCN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4092462 165419 0 None -18 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 287 3 2 4 1.8 CCCN1CCN(c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmc.2017.08.037
142590721 187053 0 None -6 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 486 9 1 3 5.2 [O-][S+](CCNC1CCN(Cc2ccc(F)cc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
CHEMBL4750660 187053 0 None -6 3 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 486 9 1 3 5.2 [O-][S+](CCNC1CCN(Cc2ccc(F)cc2)CC1)C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.ejmech.2020.112674
44431474 94258 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
CHEMBL233404 94258 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 358 4 1 2 4.5 Cc1cccc(CN2CCC(NC(=O)c3cccc4ccccc34)CC2)c1 10.1016/j.bmcl.2006.12.106
57393628 76088 0 None -229 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928137 76088 0 None -229 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
440229 94286 53 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL2334891 94286 53 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human dopamine D4 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
10895106 39001 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
CHEMBL140968 39001 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm0611152
44335979 11876 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
CHEMBL105595 11876 0 None 8 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.4 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)CC2 10.1016/s0960-894x(02)00655-8
127052458 147518 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 147518 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
22727322 20710 0 None -32 3 Human 6.1 pKi = 6.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL1196566 20710 0 None -32 3 Human 6.1 pKi = 6.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
CHEMBL557409 20710 0 None -32 3 Human 6.1 pKi = 6.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 421 9 0 6 4.5 COc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1OC 10.1016/s0960-894x(02)00179-8
154706030 183324 1 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4580817 183324 1 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597188 183324 1 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
127052458 147518 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818056 147518 0 None -77 7 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 295 5 1 3 3.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(O)cc1 10.1016/j.bmc.2016.05.053
44340376 117423 0 None 6 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325818 117423 0 None 6 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
10895106 39001 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL140968 39001 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
72164182 98925 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420777 98925 0 None -1 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4 receptor by radioligand binding assayBinding affinity to human dopamine D4 receptor by radioligand binding assay
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
25072946 118561 0 None -12 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2c(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cccc12 10.1021/jm5004039
CHEMBL3287400 118561 0 None -12 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2c(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cccc12 10.1021/jm5004039
44405530 148090 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
CHEMBL383383 148090 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cellsDisplacement of [3H]spiperone from cloned human dopamine D4.2 receptor in HEK298 cells
ChEMBL 446 6 1 4 5.3 O=C(N[C@H]1CCN(Cc2ccc(OC(F)(F)F)cc2)C1)c1ccc(-c2cccs2)cc1 10.1016/j.bmcl.2005.08.051
56837419 76079 0 None -338 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928128 76079 0 None -338 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
15888352 130891 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 369 4 0 3 3.7 CN1C(=O)c2ccccc2C1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00252-2
CHEMBL36337 130891 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 369 4 0 3 3.7 CN1C(=O)c2ccccc2C1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(98)00252-2
90644066 118817 0 None 17 4 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 5 0 3 4.8 Clc1ccc(N2CCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289653 118817 0 None 17 4 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 354 5 0 3 4.8 Clc1ccc(N2CCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
5280343 195054 124 None 1 31 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
CHEMBL1520590 195054 124 None 1 31 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
CHEMBL50 195054 124 None 1 31 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/np1000329
44591086 196360 0 None -61 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 10.1016/j.bmc.2008.12.054
CHEMBL514590 196360 0 None -61 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 10.1016/j.bmc.2008.12.054
44395709 181677 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL456429 181677 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
CHEMBL556361 181677 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for dopamine D4 receptorBinding affinity for dopamine D4 receptor
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmcl.2004.09.046
44395709 181677 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL456429 181677 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
CHEMBL556361 181677 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 10.1016/j.bmc.2008.12.054
44436302 97409 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
CHEMBL238917 97409 0 None -1 4 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4RBinding affinity to human D4R
ChEMBL 429 7 0 6 2.4 COc1ccccc1N1CCN(CCCCN2C(=O)c3ccccc3S2(=O)=O)CC1 10.1016/j.bmcl.2021.128028
44273896 106250 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/0960-894X(96)00198-9
CHEMBL283142 106250 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Binding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligandBinding affinity at cloned human Dopamine receptor D4 expressed in HEK 293 cells, using [3H]nemonapride as radioligand
ChEMBL 351 6 1 3 3.4 CC(C)(C)C(=O)NCCCCN1CCN(c2ccccc2Cl)CC1 10.1016/0960-894X(96)00198-9
9888211 28188 13 None -100 10 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
CHEMBL131495 28188 13 None -100 10 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 417 6 1 3 4.5 O=C1c2ccccc2C(=O)N1CCCCN1CC=C(c2c[nH]c3ccc(F)cc23)CC1 10.1021/jm070516u
11347425 211898 3 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
CHEMBL77850 211898 3 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 310 3 1 3 3.0 Fc1ccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)cc1 10.1021/jm0305669
12997412 15964 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
CHEMBL110349 15964 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 411 6 1 3 4.2 O=C(NCCCN1CCN(c2ccccc2)CC1)c1cccc2c1Cc1ccccc1-2 10.1021/jm010146o
11168182 10307 25 None -125 13 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
264 10307 25 None -125 13 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
CHEMBL1181770 10307 25 None -125 13 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpirideBinding affinity towards human dopamine receptor D4 expressed in CHO cells using the radioligand [125I]iodosulpiride
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
57326584 80840 0 None -8 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 396 1 0 5 4.9 Clc1ccc2c(c1)N=C(N1CCN(C3CCCCC3)CC1)c1cccnc1O2 10.1021/jm2013419
CHEMBL2022273 80840 0 None -8 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 396 1 0 5 4.9 Clc1ccc2c(c1)N=C(N1CCN(C3CCCCC3)CC1)c1cccnc1O2 10.1021/jm2013419
44394618 72965 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2004.07.045
CHEMBL184388 72965 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cellsAbility to displace [3H]spiperone from human Dopamine receptor D4.2 stably transfected in human embryonic kidney 298 cells
ChEMBL 374 5 1 2 4.5 O=C(NC1CCN(Cc2ccccc2)C1)c1ccc(-c2ccc(F)cc2)cc1 10.1016/j.bmcl.2004.07.045
44335918 11909 0 None 61 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 407 5 0 5 2.2 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
CHEMBL105745 11909 0 None 61 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 407 5 0 5 2.2 COC(=O)[C@@H]1Cc2ccccc2N1C(=O)CN1CCN(Cc2ccc(C)cc2)CC1 10.1016/s0960-894x(02)00656-x
233952 206478 17 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
CHEMBL59324 206478 17 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligandBinding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm9600712
44335876 11828 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 4 0 3 3.4 Cc1ccc(C)c(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
CHEMBL105304 11828 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 377 4 0 3 3.4 Cc1ccc(C)c(CN2CCN(CC(=O)N3c4ccccc4CC3C)CC2)c1 10.1016/s0960-894x(02)00655-8
44336314 116418 0 None 204 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 5 0 3 3.0 O=C1Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL322326 116418 0 None 204 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human dopamine D4 receptor was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 369 5 0 3 3.0 O=C1Cc2ccccc2N1CCN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
233952 206478 17 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
CHEMBL59324 206478 17 None 15 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
ChEMBL 291 3 1 2 3.5 c1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1021/jm0002432
11739255 86793 0 None 8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
CHEMBL212861 86793 0 None 8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 338 6 0 5 3.0 CO/N=C(\CCN1CCN(c2ccccn2)CC1)c1cccc(C)c1 10.1021/jm060279f
10425450 6989 30 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
3301 6989 30 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
CHEMBL375596 6989 30 None -1 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 10.1021/jm060662k
15840856 106605 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 358 5 0 3 4.7 COc1ccccc1N1CCN(Cc2cccc(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
CHEMBL285577 106605 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cellsDisplacement of [3H]YM-09151-2 from human Dopamine receptor D4.2 expressed in baculovirus Sf9 cells
ChEMBL 358 5 0 3 4.7 COc1ccccc1N1CCN(Cc2cccc(-c3ccccc3)c2)CC1 10.1016/S0960-894X(97)00218-7
44436596 98771 1 None 3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1ccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241631 98771 1 None 3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 401 5 1 3 3.5 C#Cc1ccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
10359736 106290 0 None 316 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm981041x
CHEMBL283353 106290 0 None 316 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand.
ChEMBL 337 6 1 3 3.0 CCC(C)(C)C(=O)NCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm981041x
137655735 165771 0 None -11 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4096353 165771 0 None -11 5 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
22100943 109912 0 None 41 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1cccc(CN2CC=C(c3nc4ccccc4s3)CC2)c1 10.1016/S0960-894X(97)00402-2
CHEMBL307869 109912 0 None 41 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1cccc(CN2CC=C(c3nc4ccccc4s3)CC2)c1 10.1016/S0960-894X(97)00402-2
119570 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
2233 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
953 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
CHEMBL301265 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
DB00413 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandHigh binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
119570 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
2233 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
953 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
CHEMBL301265 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
DB00413 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsHigh inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
91864602 147516 0 None -7 8 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 147516 0 None -7 8 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
10318141 213869 0 None 120 3 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C(F)(F)F)cc1)CC3 10.1021/jm970170v
CHEMBL91938 213869 0 None 120 3 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 389 3 0 4 4.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C(F)(F)F)cc1)CC3 10.1021/jm970170v
10318141 213869 0 None 120 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 389 3 0 4 4.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C(F)(F)F)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL91938 213869 0 None 120 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 389 3 0 4 4.4 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(C(F)(F)F)cc1)CC3 10.1016/j.ejmech.2020.113034
12888943 16341 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)NC2CCN(Cc3ccccc3)CC2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL112395 16341 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)NC2CCN(Cc3ccccc3)CC2)cc1Cl 10.1016/s0960-894x(03)00678-4
25131876 92967 0 None -12 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2020.113141
CHEMBL2312227 92967 0 None -12 7 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 419 9 1 5 4.0 COc1ccccc1OCCNCC1COCC(c2ccccc2)(c2ccccc2)O1 10.1016/j.ejmech.2020.113141
137640189 163732 0 None -10 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4072780 163732 0 None -10 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
10737474 108130 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
CHEMBL296953 108130 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligandBinding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand
ChEMBL 363 4 1 3 3.5 O=C(NCN1CCN(c2ccccc2Cl)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2005.02.012
53363199 70626 0 None 10 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 0 9 3.2 CCOCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803051 70626 0 None 10 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 481 12 0 9 3.2 CCOCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
22100957 211045 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 358 3 0 3 5.4 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4o3)CC2)cc1 10.1016/S0960-894X(97)00402-2
CHEMBL71208 211045 4 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 358 3 0 3 5.4 Clc1ccc(CN2CC=C(c3nc4cc(Cl)ccc4o3)CC2)cc1 10.1016/S0960-894X(97)00402-2
10620139 213553 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 385 4 0 5 4.0 COc1cc2oc(=O)c3c(c2cc1OC)CCN(Cc1ccc(Cl)cc1)C3 10.1021/jm970170v
CHEMBL90173 213553 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 385 4 0 5 4.0 COc1cc2oc(=O)c3c(c2cc1OC)CCN(Cc1ccc(Cl)cc1)C3 10.1021/jm970170v
9945233 211871 1 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
CHEMBL77563 211871 1 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccccc1N1CCN(Cc2nc3ccccc3[nH]2)CC1 10.1021/jm0305669
119570 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2233 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
953 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
CHEMBL301265 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
DB00413 9933 96 None -6 39 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130)
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2812861 215220 6 None 177 3 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4ccccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
CHEMBL99967 215220 6 None 177 3 Human 8.1 pKi = 8.1 Binding
Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151Binding affinity on human Dopamine receptor D4 expressed in CHO cells using radioligand [3H]-YM 09151
ChEMBL 319 4 1 4 2.8 c1ccc(-c2nc(CN3CCN(c4ccccn4)CC3)c[nH]2)cc1 10.1021/jm960637m
10324985 83556 8 None -6 17 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 83556 8 None -6 17 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 83556 8 None -6 17 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
2389 10104 118 None -22 66 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
5073 10104 118 None -22 66 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
96 10104 118 None -22 66 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
CHEMBL85 10104 118 None -22 66 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
DB00734 10104 118 None -22 66 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
2 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
54562 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
CHEMBL240773 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
2 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
54562 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
CHEMBL240773 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
2 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
54562 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
CHEMBL240773 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
2 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
54562 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
CHEMBL240773 10035 23 None -2 28 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
44284013 146008 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
CHEMBL37885 146008 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
10450880 213943 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
CHEMBL92373 213943 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1021/jm970170v
10685891 18369 1 None -7 5 Human 8.1 pKi = 8.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL1180627 18369 1 None -7 5 Human 8.1 pKi = 8.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@H](CNCc1ccccc1)O2 10.1021/jm9703653
CHEMBL135357 18369 1 None -7 5 Human 8.1 pKi = 8.1 Binding
Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.Binding affinity at human Dopamine receptor D4 (hD4) using [3H]spiperone radioligand.
ChEMBL 303 4 2 3 3.5 Oc1cc2c(cc1Cl)CC[C@H](CNCc1ccccc1)O2 10.1021/jm9703653
3645619 9808 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
975 9808 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
CHEMBL45244 9808 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligandBinding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
10450880 213943 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1016/j.ejmech.2020.113034
CHEMBL92373 213943 0 None 316 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 355 3 0 4 4.0 COc1ccc2c3c(c(=O)oc2c1)CN(Cc1ccc(Cl)cc1)CC3 10.1016/j.ejmech.2020.113034
57401820 76936 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940409 76936 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57401820 76936 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940409 76936 0 None 6 7 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
118709175 120200 0 None -4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 474 10 0 5 4.9 CN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318848 120200 0 None -4 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 474 10 0 5 4.9 CN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
3645619 9808 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
975 9808 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
CHEMBL45244 9808 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity of compound towards human dopamine receptor D4 was determinedBinding affinity of compound towards human dopamine receptor D4 was determined
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/j.bmcl.2005.02.012
44323780 119352 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
CHEMBL330108 119352 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Affinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperoneAffinity towards human Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1016/s0960-894x(98)00474-0
9819770 147863 10 None 208 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/j.ejmech.2020.113141
CHEMBL38262 147863 10 None 208 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to D4R (unknown origin) assessed as inhibition constantBinding affinity to D4R (unknown origin) assessed as inhibition constant
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/j.ejmech.2020.113141
44323780 119352 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
CHEMBL330108 119352 0 None 20 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Homo sapiens (human) dopamine D4.4 receptorBinding affinity to Homo sapiens (human) dopamine D4.4 receptor
ChEMBL 341 3 1 3 3.2 O=C1Cc2c(ccc(Cl)c2N2CCN(Cc3ccccc3)CC2)N1 10.1007/s00044-012-0055-5
44222483 203030 0 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
CHEMBL561763 203030 0 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 409 7 1 6 3.0 CSc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm900690y
9819770 147863 10 None 208 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL38262 147863 10 None 208 3 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
137653577 165652 0 None 208 3 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 349 4 1 3 3.6 Cc1ccc(N2CCN(CCC3C(=O)Nc4ccccc43)CC2)cc1C 10.1021/acs.jmedchem.7b00151
CHEMBL4095082 165652 0 None 208 3 Human 8.1 pKi = 8.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 349 4 1 3 3.6 Cc1ccc(N2CCN(CCC3C(=O)Nc4ccccc43)CC2)cc1C 10.1021/acs.jmedchem.7b00151
44360992 126182 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm025558r
CHEMBL344677 126182 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm025558r
228 7233 28 None -1 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
33 7233 28 None -1 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
6005 7233 28 None -1 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
CHEMBL53 7233 28 None -1 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
DB00714 7233 28 None -1 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060662k
13091359 120316 0 None -12 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321790 120316 0 None -12 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
681 8247 72 None -2 38 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
940 8247 72 None -2 38 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
947 8247 72 None -2 38 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
CHEMBL59 8247 72 None -2 38 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
DB00988 8247 72 None -2 38 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
44360992 126182 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm0611152
CHEMBL344677 126182 0 None 2 6 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm0611152
CHEMBL5278957 200784 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constantDisplacement of [3H]-methylspiperone from D4 (unknown origin) receptor expressed in HEK293T cells assessed as inhibition constant
ChEMBL 363 3 2 2 3.4 CC(C)N1C[C@H](C)[C@H](NC(=O)c2cc3ccc(Br)cc3[nH]2)C1 10.1016/j.ejmech.2020.113141
11776546 210015 2 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
CHEMBL64508 210015 2 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(98)00014-6
11776546 210015 2 None -7 6 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(99)00434-5
CHEMBL64508 210015 2 None -7 6 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranesInhibition of [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cell membranes
ChEMBL 243 6 2 3 2.6 Oc1cccc(OCCNCc2ccccc2)c1 10.1016/s0960-894x(99)00434-5
10392655 207044 0 None -380 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1016/j.bmcl.2003.09.083
CHEMBL59713 207044 0 None -380 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for human dopamine receptor D4 using [125I]IABN as radioligandBinding affinity for human dopamine receptor D4 using [125I]IABN as radioligand
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1016/j.bmcl.2003.09.083
10392655 207044 0 None -380 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assayBinding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assay
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1021/jm301545c
CHEMBL59713 207044 0 None -380 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assayBinding affinity to dopamine D4 receptor (unknown origin) by radioligand binding assay
ChEMBL 543 9 1 5 5.1 COc1cc(Br)cc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1OC 10.1021/jm301545c
72205046 98722 0 None -8 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 394 7 0 4 4.7 Clc1ccc(-n2cc(CCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
CHEMBL2414357 98722 0 None -8 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human D4 receptor after 120 mins by liquid scintillation counting
ChEMBL 394 7 0 4 4.7 Clc1ccc(-n2cc(CCCCN3CCN(c4ccccc4)CC3)cn2)cc1 10.1016/j.ejmech.2013.05.027
122177643 127989 0 None -501 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577344 127989 0 None -501 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
11452692 65686 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1021/jm101323b
CHEMBL1688991 65686 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1021/jm101323b
11452692 65686 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL1688991 65686 0 None -338 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 413 10 1 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(CCF)cc2)CC1 10.1016/j.bmcl.2014.12.023
155512662 176434 2 None -1621 3 Human 6.1 pKi = 6.1 Binding
Displacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysisDisplacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysis
ChEMBL 444 8 1 5 4.6 N#Cc1cccc(N2CCN(CCCCNC(=O)c3ccc(-c4ccsc4)cc3)CC2)c1 10.1016/j.bmcl.2019.07.020
CHEMBL4437341 176434 2 None -1621 3 Human 6.1 pKi = 6.1 Binding
Displacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysisDisplacement of 2,3-dimethoxy-5-[125I]-iodo-N-[9-benzyl-9-azabicyclo[3.3.1]nonan-3beta-yl]benzamide from dopamine human D4 receptor expressed in HEK293 cells measured after 60 mins by gamma counting analysis
ChEMBL 444 8 1 5 4.6 N#Cc1cccc(N2CCN(CCCCNC(=O)c3ccc(-c4ccsc4)cc3)CC2)c1 10.1016/j.bmcl.2019.07.020
71456890 88602 0 None -50 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1ccc2ccccc2c1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164351 88602 0 None -50 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 436 6 0 4 4.7 O=C(c1ccc2ccccc2c1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
44415689 145887 0 None -912 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL378669 145887 0 None -912 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44336004 12205 0 None 23 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 439 4 0 3 5.1 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)C(C)(C)CC2C 10.1016/s0960-894x(02)00655-8
CHEMBL107338 12205 0 None 23 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 439 4 0 3 5.1 Cc1ccc2c(c1)N(C(=O)CN1CCN(Cc3ccc(Cl)cc3)CC1)C(C)(C)CC2C 10.1016/s0960-894x(02)00655-8
242 7258 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 7258 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 7258 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 7258 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 7258 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
242 7258 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 7258 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 7258 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 7258 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 7258 124 None -104 51 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
72737767 121298 4 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
CHEMBL3335540 121298 4 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
ChEMBL 315 5 0 2 4.2 Clc1ccc(CN2CCOC(CCc3ccccc3)C2)cc1 10.1021/ml500267c
134144304 161272 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3952251 161272 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3990525 161272 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
44283963 146965 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
CHEMBL38046 146965 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 394 6 2 4 3.7 OCc1ccc(N2CCN(CC[C@@H](O)c3ccc(Cl)cc3)CC2)cc1Cl 10.1016/s0960-894x(98)00252-2
2274 9947 58 None -56 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 9947 58 None -56 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 9947 58 None -56 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 9947 58 None -56 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 9947 58 None -56 31 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
154705015 183293 1 None -186 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4454380 183293 1 None -186 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596929 183293 1 None -186 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
71062829 166913 0 None -1 3 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1ccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)nc1 nan
CHEMBL4108986 166913 0 None -1 3 Mouse 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 339 6 0 5 2.2 c1ccc(OC[C@H]2CN(CCN3CCc4ccccc43)CCO2)nc1 nan
44591043 183591 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2008.12.054
CHEMBL460855 183591 0 None 3 2 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation countingDisplacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 10.1016/j.bmc.2008.12.054
130431343 181295 0 None -2454 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 5 3.9 CCc1cccc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4555307 181295 0 None -2454 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 439 8 1 5 3.9 CCc1cccc(N2CCN(CCCCNC(=O)c3cn4ccccc4n3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
44454685 101828 0 None 7 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1cccc(CN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2007.12.026
CHEMBL255163 101828 0 None 7 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human dopamine D4.4 receptorBinding affinity to human dopamine D4.4 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1cccc(CN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2007.12.026
134144304 161272 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3952251 161272 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
CHEMBL3990525 161272 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting methodDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting method
ChEMBL 327 5 0 2 4.4 O=C(CCCN1CCc2ccccc2CC1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.09.019
57391895 76076 0 None -42 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928125 76076 0 None -42 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
155513053 176477 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4437912 176477 0 None 6 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 323 5 1 3 3.5 CCc1cccc(NC(=O)CN2CCC(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
11405107 205842 0 None 7 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 341 3 1 2 3.7 C(#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1)c1ccccc1 10.1016/s0960-894x(02)00316-5
CHEMBL58662 205842 0 None 7 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cellsAbility to displace [3H]spiperone radioligand from cloned human Dopamine receptor D4 in CHO cells
ChEMBL 341 3 1 2 3.7 C(#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1)c1ccccc1 10.1016/s0960-894x(02)00316-5
11808247 24847 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 24847 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 24847 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
11314005 116310 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 346 5 0 4 3.7 Cc1ncccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL322175 116310 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 346 5 0 4 3.7 Cc1ncccc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
162645252 190404 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4743284 190404 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802393 190404 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
11808247 24847 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL126667 24847 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3819366 24847 0 None 1 9 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1016/j.bmc.2016.05.053
10961938 126317 0 None -1380 7 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm050171k
CHEMBL345820 126317 0 None -1380 7 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat dopamine D4 receptor using [11C] radiotracerBinding affinity for rat dopamine D4 receptor using [11C] radiotracer
ChEMBL 485 8 1 4 5.5 COc1c(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc2ccccc12 10.1021/jm050171k
71658207 97183 0 None -46 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 460 8 1 5 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)nc2)CC1 10.1016/j.bmc.2013.03.074
CHEMBL2386621 97183 0 None -46 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysisDisplacement of [125I]ABN from human dopamine D4.4 receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
ChEMBL 460 8 1 5 3.6 COc1ccccc1N1CCCN(CCCCNC(=O)c2ccc(Br)nc2)CC1 10.1016/j.bmc.2013.03.074
4209 9937 75 None -562 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
4893 9937 75 None -562 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
503 9937 75 None -562 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
5385 9937 75 None -562 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
CHEMBL2 9937 75 None -562 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
DB00457 9937 75 None -562 33 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm020938y
127052486 147601 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819153 147601 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
46231926 207358 0 None -41686 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599135 207358 0 None -41686 4 Human 5.1 pKi = 5.1 Binding
Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation countingDisplacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
10689266 213823 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc(CN2CCc3c(c(=O)oc4cc(OC)ccc34)C2)cc1 10.1021/jm970170v
CHEMBL91658 213823 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitroAbility to displace [3H]spiperone from cloned human Dopamine receptor D4 expressed in CHO K-1 cells in vitro
ChEMBL 351 4 0 5 3.4 COc1ccc(CN2CCc3c(c(=O)oc4cc(OC)ccc34)C2)cc1 10.1021/jm970170v
10689266 213823 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 351 4 0 5 3.4 COc1ccc(CN2CCc3c(c(=O)oc4cc(OC)ccc34)C2)cc1 10.1016/j.ejmech.2020.113034
CHEMBL91658 213823 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human D4 receptor assessed as inhibition constantBinding affinity to human D4 receptor assessed as inhibition constant
ChEMBL 351 4 0 5 3.4 COc1ccc(CN2CCc3c(c(=O)oc4cc(OC)ccc34)C2)cc1 10.1016/j.ejmech.2020.113034
162645252 190404 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4743284 190404 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
CHEMBL4802393 190404 0 None -1 7 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor by liquid scintillation counting
ChEMBL 389 7 0 3 5.0 Fc1ccc(CCCCN2CCN(c3cccc(-c4ccccc4)n3)CC2)cc1 10.1016/j.bmc.2020.115943
56649649 74632 0 None -97 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910140 74632 0 None -97 8 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 480 8 0 5 4.6 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)CC3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
44431483 174424 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
CHEMBL430167 174424 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2006.12.106
137655451 165632 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4094869 165632 0 None -6 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human Dopamine D4 receptor expressed in CHO cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
56833463 75111 0 None -41 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 578 17 1 9 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916552 75111 0 None -41 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in chinese hamster CHO cells by radioligand binding assay
ChEMBL 578 17 1 9 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
11783703 47808 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 1 1 5 4.5 Cc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL148752 47808 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 375 1 1 5 4.5 Cc1ccc2c(c1)C(N1CCN(C3CCCCC3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
11560697 17382 0 None -363 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
CHEMBL1170095 17382 0 None -363 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 414 4 2 3 4.4 COc1cccc2[nH]cc(CN3CCC(O)(c4ccc(Br)cc4)CC3)c12 10.1016/j.bmc.2010.05.052
127052486 147601 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
CHEMBL3819153 147601 0 None -8 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL 424 6 1 5 4.8 O=c1[nH]c2cc(Cl)ccc2n1C1CCN(CCCCc2nc3ccccc3o2)CC1 10.1016/j.bmc.2016.06.011
154705128 183070 1 None -58 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4454872 183070 1 None -58 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595148 183070 1 None -58 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL5079903 221430 0 None -32 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysisDisplacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
ChEMBL None None None N#CC(CCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
154724609 183378 1 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4514800 183378 1 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4597637 183378 1 None -1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
154726922 183320 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4442936 183320 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597157 183320 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
118709171 120195 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1085 35 0 8 16.8 O=C(CCCCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318843 120195 0 None -2 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1085 35 0 8 16.8 O=C(CCCCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
45483655 204894 0 None -12 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7ccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)cc7)nn6)cc5)cc4)nn3)cc2)CC1 10.1021/jm901120h
CHEMBL574534 204894 0 None -12 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7ccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)cc7)nn6)cc5)cc4)nn3)cc2)CC1 10.1021/jm901120h
11151135 116194 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cellsIn vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cells
ChEMBL 313 6 0 4 3.0 COc1ccccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
CHEMBL322002 116194 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cellsIn vitro ability to inhibit binding of [3H]spiperone to human recombinant Dopamine receptor D4.2 expressed on CHO cells
ChEMBL 313 6 0 4 3.0 COc1ccccc1OCC1CN(Cc2ccccc2)CCO1 10.1021/jm031111m
154706123 183067 1 None -107 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4593394 183067 1 None -107 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595145 183067 1 None -107 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
168286314 198438 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5196213 198438 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
127035062 143229 0 None -29 19 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 143229 0 None -29 19 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
91864602 147516 0 None -7 8 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
CHEMBL3818047 147516 0 None -7 8 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat D4 receptor expressed in cell membranes after 1 hr by liquid scintillation counting
ChEMBL 313 5 0 2 4.4 O=C(CCCN1CCc2ccccc2C1)c1ccc(Cl)cc1 10.1016/j.bmc.2016.05.053
168286314 198438 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
CHEMBL5196213 198438 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.ejmech.2022.114840
168286314 198438 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5196213 198438 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 389 5 1 3 4.8 FC(F)(F)c1cccc(COC2CCN(Cc3ccc4[nH]ncc4c3)CC2)c1 10.1016/j.bmcl.2022.128615
56681925 73140 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 462 7 1 5 3.5 CN1CN(c2ccccc2)C2(CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)C1=O 10.1016/j.bmc.2011.04.021
CHEMBL1813589 73140 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 462 7 1 5 3.5 CN1CN(c2ccccc2)C2(CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)C1=O 10.1016/j.bmc.2011.04.021
CHEMBL1851628 73140 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counterDisplacement of [125I]ABN from human recombinant D4 receptor expressed in HEK cells after 60 mins by gamma counter
ChEMBL 462 7 1 5 3.5 CN1CN(c2ccccc2)C2(CCN(CCCCOc3ccc4c(c3)NC(=O)CC4)CC2)C1=O 10.1016/j.bmc.2011.04.021
44338149 117114 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 575 10 0 3 8.2 Fc1ccc(C(OCCN2C3CCC2CC(OC(c2ccc(F)cc2)c2ccc(F)cc2)C3)c2ccc(F)cc2)cc1 10.1021/jm010146o
CHEMBL323997 117114 0 None -4 3 Human 6.1 pKi = 6.1 Binding
Binding affinity at human dopamine receptor D4Binding affinity at human dopamine receptor D4
ChEMBL 575 10 0 3 8.2 Fc1ccc(C(OCCN2C3CCC2CC(OC(c2ccc(F)cc2)c2ccc(F)cc2)C3)c2ccc(F)cc2)cc1 10.1021/jm010146o
44360984 41855 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm025558r
CHEMBL143352 41855 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm025558r
44316315 212298 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)
ChEMBL 215 2 0 3 2.1 CCCN1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL80845 212298 0 None -5 5 Human 7.1 pKi = 7.1 Binding
Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 87/23000)
ChEMBL 215 2 0 3 2.1 CCCN1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
10623982 213831 0 None 7 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 463 7 2 4 4.6 COc1cc(NC(=O)c2ccccc2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
CHEMBL91693 213831 0 None 7 2 Human 7.1 pKi = 7.1 Binding
Binding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
ChEMBL 463 7 2 4 4.6 COc1cc(NC(=O)c2ccccc2)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C1 10.1021/jm9601720
22100965 210539 4 None 16 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccccc1CN1CC=C(c2nc3ccccc3s2)CC1 10.1016/S0960-894X(97)00402-2
CHEMBL67982 210539 4 None 16 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 340 3 0 3 5.2 Clc1ccccc1CN1CC=C(c2nc3ccccc3s2)CC1 10.1016/S0960-894X(97)00402-2
44372154 60999 0 None 11 4 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 434 4 0 4 5.4 Cc1nn2c(-c3ccc(F)cc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160749 60999 0 None 11 4 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 434 4 0 4 5.4 Cc1nn2c(-c3ccc(F)cc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
44360984 41855 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm0611152
CHEMBL143352 41855 0 None -7 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm0611152
16007117 86811 0 None -870 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212912 86811 0 None -870 6 Human 6.1 pKi = 6.1 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
137660707 166078 0 None -281 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 463 7 2 7 3.4 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4099666 166078 0 None -281 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 463 7 2 7 3.4 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5oc(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
118719795 122500 0 None -234 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 442 8 0 7 4.0 COc1ccccc1N1CCN(CCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353898 122500 0 None -234 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 442 8 0 7 4.0 COc1ccccc1N1CCN(CCCCc2cn(-c3cccc4cnccc34)nn2)CC1 10.1016/j.bmcl.2014.12.023
154725749 183467 1 None -79 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4453478 183467 1 None -79 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598388 183467 1 None -79 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
11849229 144952 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
CHEMBL376955 144952 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 349 7 0 6 2.5 N#CCO/N=C(\CCN1CCN(c2ccccn2)CC1)c1ccccc1 10.1021/jm060279f
22727347 19802 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 417 9 0 5 5.0 COc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL1189897 19802 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 417 9 0 5 5.0 COc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
CHEMBL539744 19802 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 417 9 0 5 5.0 COc1ccccc1N1CCN(CCCCc2cc(/C=C/c3ccccc3)no2)CC1 10.1016/s0960-894x(02)00179-8
11775107 172995 0 None 22 2 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
CHEMBL426629 172995 0 None 22 2 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1cccc2c1N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
863787 73065 13 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
CHEMBL184772 73065 13 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 339 5 1 4 2.8 COc1ccc(N2CCN(CC(=O)Nc3cccc(C)c3)CC2)cc1 10.1016/j.bmcl.2004.07.068
164610259 191886 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 480 6 2 4 4.7 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Br)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4856161 191886 0 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 480 6 2 4 4.7 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1Br)CC2 10.1016/j.bmcl.2021.128047
49782841 24424 0 None -549 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.1 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccccc2s1 10.1021/jm100899z
CHEMBL1258382 24424 0 None -549 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.1 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccccc2s1 10.1021/jm100899z
137642033 164923 0 None -147 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 291 3 2 5 1.3 CCCN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4087217 164923 0 None -147 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranesDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes
ChEMBL 291 3 2 5 1.3 CCCN1CCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
44438237 100434 2 None -47 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
CHEMBL246855 100434 2 None -47 3 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cellsDisplacement of [125I]IABN from human dopamine D4 receptor expressed in HEK293 cells
ChEMBL 424 8 1 3 6.4 CCCCCCn1cc(CN2CCC(O)(c3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2006.10.076
127053222 146147 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
CHEMBL3793072 146147 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 369 5 0 3 4.1 Fc1ccc(CN2CCO[C@H](COc3ccccc3)C2)cc1C(F)(F)F 10.1016/j.bmcl.2016.03.102
57398352 76937 0 None 6 5 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 398 6 0 3 5.1 Fc1ccc(SCCCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940410 76937 0 None 6 5 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 398 6 0 3 5.1 Fc1ccc(SCCCN2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
90644228 118563 0 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287402 118563 0 None -14 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
118709177 120202 0 None -17 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1135 31 0 14 12.5 O=C(CCc1cn(CCCCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318850 120202 0 None -17 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 1135 31 0 14 12.5 O=C(CCc1cn(CCCCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
135442113 125770 0 None 2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 2 5 5.1 Clc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
CHEMBL342536 125770 0 None 2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranesIn vitro binding affinity at human cloned Dopamine receptor D4 expressed in Sf9 cell membranes
ChEMBL 417 3 2 5 5.1 Clc1ccc2c(c1)C(NC1CCN(Cc3ccccc3)CC1)=Nc1cccnc1N2 10.1021/jm0104825
155533824 178677 0 None -27 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 238 2 0 2 2.7 CCc1cccc(N2CCN(C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4469777 178677 0 None -27 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysisDisplacement of [3H]N-methylspiperone from human dopamine D4.4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting analysis
ChEMBL 238 2 0 2 2.7 CCc1cccc(N2CCN(C)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
51353676 66955 0 None -1380 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 442 11 1 5 3.4 CN(C)c1ccc(C(=O)NCCCCN2CCN(c3ccccc3OCCF)CC2)cc1 10.1021/jm101323b
CHEMBL1689002 66955 0 None -1380 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 442 11 1 5 3.4 CN(C)c1ccc(C(=O)NCCCCN2CCN(c3ccccc3OCCF)CC2)cc1 10.1021/jm101323b
CHEMBL1739784 66955 0 None -1380 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 442 11 1 5 3.4 CN(C)c1ccc(C(=O)NCCCCN2CCN(c3ccccc3OCCF)CC2)cc1 10.1021/jm101323b
51353992 66985 0 None -812 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 443 11 1 4 3.7 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(CCF)cc1 10.1021/jm101323b
CHEMBL1689009 66985 0 None -812 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 443 11 1 4 3.7 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(CCF)cc1 10.1021/jm101323b
CHEMBL1739965 66985 0 None -812 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 443 11 1 4 3.7 O=C(NC/C=C/CN1CCN(c2ccccc2OCCF)CC1)c1ccc(CCF)cc1 10.1021/jm101323b
9980998 37808 0 None -524 7 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm020952a
CHEMBL139926 37808 0 None -524 7 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm020952a
CHEMBL2112911 37808 0 None -524 7 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm020952a
9980998 37808 0 None -524 7 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 37808 0 None -524 7 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 37808 0 None -524 7 Human 6.1 pKi = 6.1 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in Sf9 cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
53248365 68860 0 None -933 7 Human 6.1 pKi = 6.1 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
CHEMBL1774995 68860 0 None -933 7 Human 6.1 pKi = 6.1 Binding
Inhibition of dopamine D4 receptorInhibition of dopamine D4 receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
53326601 65685 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1021/jm101323b
CHEMBL1688990 65685 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1021/jm101323b
53326601 65685 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL1688990 65685 0 None -1122 4 Human 6.1 pKi = 6.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 410 9 1 5 3.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(N(C)C)cc2)CC1 10.1016/j.bmcl.2014.12.023
135398737 7745 93 None -7 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 7745 93 None -7 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 7745 93 None -7 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 7745 93 None -7 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 7745 93 None -7 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
3645619 9808 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4Binding affinity towards cloned human Dopamine receptor D4
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/s0960-894x(00)00633-8
975 9808 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4Binding affinity towards cloned human Dopamine receptor D4
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/s0960-894x(00)00633-8
CHEMBL45244 9808 20 None -5 9 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Dopamine receptor D4Binding affinity towards cloned human Dopamine receptor D4
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1016/s0960-894x(00)00633-8
10950176 51786 1 None 13 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 435 8 1 4 4.3 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
CHEMBL152391 51786 1 None 13 3 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligandBinding affinity towards human Dopamine receptor D4 using [3H]spiroperidol as radioligand
ChEMBL 435 8 1 4 4.3 COc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1021/jm020952a
155530733 178358 0 None 9 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 5 3.9 COc1ccccc1N1CCN(CCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4465002 178358 0 None 9 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 5 3.9 COc1ccccc1N1CCN(CCNC(=O)NN(Cc2ccccc2)c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
10158455 126748 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 409 3 0 3 3.8 CC1Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
CHEMBL349833 126748 0 None 15 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from D4 receptorDisplacement of [3H]-YM 09151 from D4 receptor
ChEMBL 409 3 0 3 3.8 CC1Cc2cccc3c2N1C(=O)C(N1CCN(Cc2ccc(Cl)cc2)CC1)CC3 10.1016/s0960-894x(02)01056-9
10495652 43349 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 316 4 0 2 4.9 c1ccc(C2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
CHEMBL144835 43349 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
ChEMBL 316 4 0 2 4.9 c1ccc(C2CCN(Cc3ccn(-c4ccccc4)c3)CC2)cc1 10.1021/jm00025a013
1613 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
205 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
3964 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
CHEMBL831 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
DB00408 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1021/jm2013419
163091 7282 34 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
22 7282 34 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
CHEMBL504548 7282 34 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]N-methylspiperone from human D4 dopamine receptor incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
10643780 126173 0 None 97 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL344602 126173 0 None 97 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)[nH]c2c1 10.1021/jm0009989
10594113 211689 1 None 13 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
CHEMBL76090 211689 1 None 13 3 Human 8.0 pKi = 8.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 351 4 1 2 5.1 Clc1ccc(-c2cc(C3CCN(Cc4ccccc4)CC3)[nH]n2)cc1 10.1021/jm970111h
11131951 56695 1 None -363 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm100925m
CHEMBL156845 56695 1 None -363 4 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation countingDisplacement of [3H]MSP from rat dopamine D4 receptor expressed in HEK293 cells after 90 mins by scintillation counting
ChEMBL 353 6 1 4 2.6 COc1cccc(C(=O)NCCN2CCN(c3ccc(C)cc3)CC2)c1 10.1021/jm100925m
15467369 107705 0 None 562 3 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccccc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL293956 107705 0 None 562 3 Human 8.0 pKi = 8.0 Binding
Binding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity of compound towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccccc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
90644230 118567 0 None -4 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287406 118567 0 None -4 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
23364995 120197 0 None -2 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 417 7 0 4 5.0 CC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318845 120197 0 None -2 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assayDisplacement of [3H]spiperone from human D4.4 receptor stably expressed in CHO cell membranes by competitive binding assay
ChEMBL 417 7 0 4 5.0 CC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
11292776 12357 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
CHEMBL107691 12357 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 409 7 0 4 5.1 CCOc1ccc(Cl)cc1OCC1CN(Cc2ccc(Cl)cc2)CCCO1 10.1021/jm031111m
44283757 144640 0 None 128 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 348 4 1 2 4.4 Cc1ccc(C2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL37604 144640 0 None 128 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement.
ChEMBL 348 4 1 2 4.4 Cc1ccc(C2CCN(CCC3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
57345617 77231 0 None 1 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
CHEMBL1946123 77231 0 None 1 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]-N-methylspiperone from rat dopamine D4 receptorDisplacement of [3H]-N-methylspiperone from rat dopamine D4 receptor
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmc.2012.01.022
127028505 146111 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
CHEMBL3792731 146111 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cellsDisplacement of [3H]-Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells
ChEMBL 333 5 0 3 4.3 Clc1ccc(CN2CCO[C@H](CSc3ccccc3)C2)cc1 10.1016/j.bmcl.2016.03.102
76518514 120314 0 None 1 9 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321788 120314 0 None 1 9 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 387 6 1 2 5.3 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCCc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
122177645 127991 0 None -44 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577346 127991 0 None -44 6 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
10356955 19760 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 291 1 0 2 4.7 CN1CCC(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL1189601 19760 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 291 1 0 2 4.7 CN1CCC(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
CHEMBL539057 19760 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Ability to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cellsAbility to inhibit the binding of [3H]spiperone to the Dopamine receptor D4 in COS7 cells
ChEMBL 291 1 0 2 4.7 CN1CCC(C2=Cc3ccccc3Oc3ccccc32)CC1 10.1021/jm00004a016
57398351 76933 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940406 76933 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assayDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
57398351 76933 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
CHEMBL1940406 76933 0 None 4 7 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation countingDisplacement of [3H]N-methylspiperone from rat dopamine D4 receptor by liquid scintillation counting
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2011.12.019
11504230 84992 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL210567 84992 0 None -12 7 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 receptor expressed in CHO cells
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
71461481 90845 0 None 8 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 356 4 0 3 4.1 C#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
CHEMBL2207632 90845 0 None 8 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 356 4 0 3 4.1 C#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
76321556 113154 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 113154 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 113154 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
2099556 211832 7 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
CHEMBL77151 211832 7 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement.
ChEMBL 326 3 1 3 3.5 Clc1cccc(N2CCN(Cc3nc4ccccc4[nH]3)CC2)c1 10.1021/jm0305669
155566403 182715 0 None 52 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 4 4.8 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
CHEMBL4587645 182715 0 None 52 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 477 9 2 4 4.8 O=C(NCCCN1CCN(c2ccc(Cl)cc2)CC1)NN(Cc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01085
76321556 113154 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 113154 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 113154 0 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]spiperone from human dopamine D4 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
54585810 68378 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3c(cccc3-c3ccccc3)C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771108 68378 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3c(cccc3-c3ccccc3)C2=O)CC1 10.1016/j.bmcl.2010.12.083
44403225 77323 0 None 5 5 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 421 9 1 5 2.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL194755 77323 0 None 5 5 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 421 9 1 5 2.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
9129986 11830 1 None 67 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
CHEMBL105317 11830 1 None 67 2 Human 8.0 pKi = 8 Binding
Binding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine type 4 receptor was determined by competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 379 5 0 4 2.8 COc1ccc(CN2CCN(CC(=O)N3c4ccccc4C[C@H]3C)CC2)cc1 10.1016/s0960-894x(02)00656-x
44412268 85142 9 None 47 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL211026 85142 9 None 47 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1016/j.bmcl.2006.02.075
25142456 89181 2 None -44 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 89181 2 None -44 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned dopamine D4 receptorBinding affinity to human cloned dopamine D4 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
11849268 175576 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(/CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
CHEMBL437532 175576 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A-369508 from human recombinant D4.4 receptor expressed in HEK293 cell membrane
ChEMBL 357 6 0 4 4.4 CO/N=C(/CCN1CCC(c2ccccn2)CC1)c1ccc(Cl)cc1 10.1021/jm060279f
118719797 122502 0 None -12 4 Human 7.1 pKi = 7.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 459 8 0 7 4.8 COc1ccccc1N1CCN(CCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
CHEMBL3353900 122502 0 None -12 4 Human 7.1 pKi = 7.1 Binding
Displacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assayDisplacement of of [125I]-IABN from human D4 receptor expressed in HEK293 cell membranes after 60 mins by filtration binding assay
ChEMBL 459 8 0 7 4.8 COc1ccccc1N1CCN(CCCc2cn(-c3ccc(-c4ccsc4)cc3)nn2)CC1 10.1016/j.bmcl.2014.12.023
71086428 158332 0 None 66 2 Mouse 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3963122 158332 0 None 66 2 Mouse 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
8704110 73375 9 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
CHEMBL185263 73375 9 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]6b binding to human Dopamine receptor D4.4
ChEMBL 327 4 1 3 2.9 Cc1cccc(NC(=O)CN2CCN(c3ccc(F)cc3)CC2)c1 10.1016/j.bmcl.2004.07.068
127698 122778 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00026a007
CHEMBL335545 122778 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperoneBinding affinity towards human Dopamine receptor D4.2 evaluated using [3H]spiperone
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00026a007
127698 122778 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Tested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligandTested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligand
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00047a010
CHEMBL335545 122778 6 None -6 4 Human 7.0 pKi = 7.0 Binding
Tested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligandTested for binding affinity towards human Dopamine receptor D4.2 using [3H]spiperone as radioligand
ChEMBL 329 4 0 1 5.7 C1=C(c2ccccc2)CCN(C[C@@H]2CCC=C(c3ccccc3)C2)C1 10.1021/jm00047a010
127046949 146687 0 None -141 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799455 146687 0 None -141 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
135398737 7745 93 None -13 90 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
38 7745 93 None -13 90 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
722 7745 93 None -13 90 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
CHEMBL42 7745 93 None -13 90 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
DB00363 7745 93 None -13 90 Human 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligandBinding affinity towards Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as the competitive ligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00656-x
11630058 148153 0 None -7 2 Human 4.1 pKi = 4.1 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 237 4 1 5 1.0 CCCNC1CCn2ncc(C(=O)OC)c2C1 10.1021/jm0503805
CHEMBL383805 148153 0 None -7 2 Human 4.1 pKi = 4.1 Binding
Binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligandBinding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand
ChEMBL 237 4 1 5 1.0 CCCNC1CCn2ncc(C(=O)OC)c2C1 10.1021/jm0503805
142590701 186300 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 484 8 1 3 5.8 O=C(c1ccc(F)cc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
CHEMBL4741279 186300 0 None -1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 484 8 1 3 5.8 O=C(c1ccc(F)cc1)N1CCC(NCCSC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.ejmech.2020.112674
132060720 169268 0 None -2 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL4167315 169268 0 None -2 9 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human dopamine D4 expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 315 4 0 2 4.9 COc1cccc(-c2ccc3c(c2)CN(Cc2ccccc2)C3)c1 10.1016/j.ejmech.2018.02.024
CHEMBL5270824 200433 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 359 5 0 5 2.9 Fc1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1F 10.1016/j.ejmech.2022.114840
CHEMBL5270824 200433 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 359 5 0 5 2.9 Fc1ccc(OC[C@@H]2CN(Cc3cn4ccccc4n3)CCO2)cc1F 10.1016/j.ejmech.2022.114840
11699516 148412 0 None -2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 540 10 1 7 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
CHEMBL385289 148412 0 None -2 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 540 10 1 7 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3Br)c2C)CC1 10.1021/jm0611152
8690650 11539 4 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 268 3 1 3 2.7 Oc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL103900 11539 4 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned Dopamine receptor D4.4 expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 268 3 1 3 2.7 Oc1ccc(N2CCN(Cc3ccccc3)CC2)cc1 10.1016/s0960-894x(98)00014-6
154726381 183306 1 None -173 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4522558 183306 1 None -173 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597048 183306 1 None -173 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
44269820 51815 0 None -2 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 369 3 0 4 4.8 CN1CCN(c2nc3ccccc3c(Cl)c2Sc2ccccc2)CC1 10.1016/s0960-894x(01)00167-6
CHEMBL15242 51815 0 None -2 3 Human 7.0 pKi = 7.0 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
ChEMBL 369 3 0 4 4.8 CN1CCN(c2nc3ccccc3c(Cl)c2Sc2ccccc2)CC1 10.1016/s0960-894x(01)00167-6
56649650 74633 0 None -104 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
CHEMBL1910141 74633 0 None -104 8 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assayDisplacement of [3H]N-methylspiperone from dopamine D4 receptor expressed in HEK293 EBNA cells by radioligand binding assay
ChEMBL 466 8 0 5 4.2 COc1ccccc1N1CCN(CCN(C(=O)C23CCC(CF)(CC2)C3)c2ccccn2)CC1 10.1016/j.ejmech.2011.06.023
9882594 117160 0 None -436 5 Human 7.0 pKi = 7.0 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)CC1c1ccccc1C2 10.1021/jm010566d
CHEMBL324270 117160 0 None -436 5 Human 7.0 pKi = 7.0 Binding
The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2
ChEMBL 294 1 0 3 3.1 COc1cccc2c1N1CCN(C)CC1c1ccccc1C2 10.1021/jm010566d
9910451 170909 0 None -912 7 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL420997 170909 0 None -912 7 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
11152225 11899 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1cc(Cl)cc(OCC2CN(Cc3ccccc3)CCO2)c1 10.1021/jm031111m
CHEMBL105690 11899 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4In vitro ability of compound to inhibit binding of [3H]spiperone to human Dopamine receptor D4
ChEMBL 347 6 0 4 3.6 COc1cc(Cl)cc(OCC2CN(Cc3ccccc3)CCO2)c1 10.1021/jm031111m
127046948 146848 0 None -398 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800468 146848 0 None -398 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
44582705 193775 0 None -5 13 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 193775 0 None -5 13 Human 6.0 pKi = 6.0 Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experimentInhibition of human cloned dopamine D4 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
9980998 37808 0 None -524 7 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
CHEMBL139926 37808 0 None -524 7 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
CHEMBL2112911 37808 0 None -524 7 Human 7.0 pKi = 7.0 Binding
Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.Binding affinity for human Dopamine receptor D4 by [3H]- spiperone displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
9928553 24212 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 354 3 0 4 3.8 O=c1ccc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2o1 10.1021/jm990266k
CHEMBL125763 24212 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cellsBinding affinity using [3H]spiperone displacement from cloned human Dopamine receptor D4.2 expressed in CHO-K1 cells
ChEMBL 354 3 0 4 3.8 O=c1ccc2ccc(CN3CCN(c4ccc(Cl)cc4)CC3)cc2o1 10.1021/jm990266k
53359025 69127 0 None 2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
CHEMBL1779058 69127 0 None 2 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cellsDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK cells
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
9980998 37808 0 None -524 7 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL139926 37808 0 None -524 7 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
CHEMBL2112911 37808 0 None -524 7 Human 7.0 pKi = 7.0 Binding
Inhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cellsInhibition of [3H]spiperone binding to human Dopamine D4 receptor expressed in CHO cells
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm040190e
9980998 37808 0 None -524 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0611152
CHEMBL139926 37808 0 None -524 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0611152
CHEMBL2112911 37808 0 None -524 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0611152
10522334 112189 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 4.6 c1ccc(CCN2CCC3(CCc4c3n[nH]c4-c3ccccc3)CC2)cc1 10.1021/jm970111h
CHEMBL311832 112189 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells.
ChEMBL 357 4 1 2 4.6 c1ccc(CCN2CCC3(CCc4c3n[nH]c4-c3ccccc3)CC2)cc1 10.1021/jm970111h
44323870 118368 0 None -9 4 Human 6.0 pKi = 6.0 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL328246 118368 0 None -9 4 Human 6.0 pKi = 6.0 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
44393737 72535 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
CHEMBL183466 72535 0 None - 1 Human 6.0 pKi = 6.0 Binding
In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4In vitro ability to inhibit [3H]spiperone binding to human Dopamine receptor D4.4
ChEMBL 646 4 1 4 5.7 Cc1c(Br)cc(Br)c(NC(=O)CN2CCN(c3ccc(Br)cc3C#N)CC2)c1Br 10.1016/j.bmcl.2004.07.068
49798799 21130 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 353 4 2 4 3.8 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2010.05.052
CHEMBL1172209 21130 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 353 4 2 4 3.8 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2010.05.052
CHEMBL1200150 21130 0 None -3 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 353 4 2 4 3.8 CSc1ccc(C2(O)CCN(Cc3c[nH]c4ncccc34)CC2)cc1 10.1016/j.bmc.2010.05.052
20256387 11544 2 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 227 6 1 2 2.9 c1ccc(CNCCOc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
CHEMBL103951 11544 2 None 1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligandBinding affinity towards human cloned dopamine (hD4.4) receptor expressed in CHO cells using [3H]spiperone as radioligand
ChEMBL 227 6 1 2 2.9 c1ccc(CNCCOc2ccccc2)cc1 10.1016/s0960-894x(98)00014-6
122181326 128645 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL3590077 128645 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assayDisplacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1021/acs.jmedchem.9b01085
137636498 162975 0 None -40 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064186 162975 0 None -40 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]spiperone from human D4R expressed in CHO cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
122181326 128645 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590077 128645 0 None -30 6 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranesDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
749986 211042 10 None 15 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 289 3 1 2 3.9 C1=C(c2nc3ccccc3[nH]2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
CHEMBL71173 211042 10 None 15 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 289 3 1 2 3.9 C1=C(c2nc3ccccc3[nH]2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
49798835 21133 0 None -14 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1172213 21133 0 None -14 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
CHEMBL1200153 21133 0 None -14 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 385 3 1 3 4.7 OC1(c2ccc(Br)cc2)CCN(Cc2coc3ccccc23)CC1 10.1016/j.bmc.2010.05.052
15508240 117304 0 None 6 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 264 3 0 2 3.3 C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL325104 117304 0 None 6 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 264 3 0 2 3.3 C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
49798857 21087 0 None -117 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 407 5 0 4 4.0 O=C1N(CCF)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1170085 21087 0 None -117 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 407 5 0 4 4.0 O=C1N(CCF)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1199947 21087 0 None -117 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 407 5 0 4 4.0 O=C1N(CCF)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
154725276 183069 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4456964 183069 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595147 183069 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
23290944 88601 0 None -323 7 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
CHEMBL2164350 88601 0 None -323 7 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM-09151-2 from human cloned D4 receptor expressed in Sf9 cells after 60 mins by liquid scintillation counting
ChEMBL 392 6 0 4 3.8 O=C(C1CCCCC1)N(CCN1CCN(c2ccccc2)CC1)c1ccccn1 10.1016/j.bmcl.2012.05.119
44336055 12122 0 None 43 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1CCc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
CHEMBL106897 12122 0 None 43 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 397 4 0 3 3.8 CC1CCc2ccccc2N1C(=O)CN1CCN(Cc2ccc(Cl)cc2)CC1 10.1016/s0960-894x(02)00655-8
145993990 174133 0 None -21 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 372 7 2 4 3.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(F)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4294577 174133 0 None -21 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranesDisplacement of [3H]N-Methylspiperone from human dopamine D4 receptor expressed in HEK cell membranes
ChEMBL 372 7 2 4 3.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(F)cc1)CC2 10.1021/acsmedchemlett.8b00229
137651576 164267 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 308 7 0 3 3.6 COc1cccc(CCC2=NCCN2CCc2ccccc2)c1 10.1016/j.ejmech.2020.113141
CHEMBL4079495 164267 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constantDisplacement of [3H]N-methylspiperone from D4 (unknown origin) receptor expressed in HEK293 cells assessed as inhibition constant
ChEMBL 308 7 0 3 3.6 COc1cccc(CCC2=NCCN2CCc2ccccc2)c1 10.1016/j.ejmech.2020.113141
155563301 182029 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4572245 182029 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting methodDisplacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method
ChEMBL 344 4 1 4 2.8 Cc1cccc(NC(=O)CN2CCN(c3ccc(Cl)cn3)CC2)c1 10.1021/acs.jmedchem.9b00231
168284020 198032 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5190239 198032 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
168284020 198032 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
CHEMBL5190239 198032 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]N-methylspiperone from human D4 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.bmcl.2022.128615
137651576 164267 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 308 7 0 3 3.6 COc1cccc(CCC2=NCCN2CCc2ccccc2)c1 10.1021/acs.jmedchem.8b00265
CHEMBL4079495 164267 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting methodDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method
ChEMBL 308 7 0 3 3.6 COc1cccc(CCC2=NCCN2CCc2ccccc2)c1 10.1021/acs.jmedchem.8b00265
164612933 191779 0 None -9 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4854512 191779 0 None -9 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 436 6 2 4 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2021.128047
164627090 193337 0 None -12 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1OC)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4878121 193337 0 None -12 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
ChEMBL 432 7 2 5 3.9 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccccc1OC)CC2 10.1016/j.bmcl.2021.128047
9843032 115310 0 None 45 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.6 CC1CN(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
CHEMBL320067 115310 0 None 45 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 383 4 0 3 3.6 CC1CN(C(=O)CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/s0960-894x(02)00655-8
168284020 198032 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
CHEMBL5190239 198032 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membraneDisplacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane
ChEMBL 387 5 0 4 4.6 Cc1nc(CN2CCC(OCc3ccc(Cl)c(F)c3)CC2)c2ccccn12 10.1016/j.ejmech.2022.114840
44431468 95045 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
CHEMBL234824 95045 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nemonapride from human cloned dopamine D4.2 receptorDisplacement of [3H]nemonapride from human cloned dopamine D4.2 receptor
ChEMBL 412 4 1 2 5.3 O=C(NC1CCN(Cc2ccc(C(F)(F)F)cc2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2006.12.106
10110263 19764 1 None -7 3 Human 7.0 pKi = 7.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 379 7 0 4 4.6 Fc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL1189648 19764 1 None -7 3 Human 7.0 pKi = 7.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 379 7 0 4 4.6 Fc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
CHEMBL539235 19764 1 None -7 3 Human 7.0 pKi = 7.0 Binding
Displacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cellsDisplacement of the radioligand [3H]spiperone from the cloned human dopamine receptor D4 expressed in CHO cells
ChEMBL 379 7 0 4 4.6 Fc1ccc(-c2cc(CCCCN3CCN(c4ccccc4)CC3)on2)cc1 10.1016/s0960-894x(02)00179-8
15508242 172028 0 None 32 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
CHEMBL422959 172028 0 None 32 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cellsDisplacement of [3H]spiperone from human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 268 4 0 3 3.1 O=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
45270813 203468 0 None -112 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)nc(C)n34)CC2)cc1 10.1016/j.bmc.2009.05.015
CHEMBL564709 203468 0 None -112 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells
ChEMBL 365 4 0 6 3.0 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)nc(C)n34)CC2)cc1 10.1016/j.bmc.2009.05.015
154704418 183366 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4546749 183366 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4597533 183366 1 None -2 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
12581203 31845 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 233 4 0 2 2.9 CCN(CC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
CHEMBL134701 31845 0 None -7 3 Human 6.0 pKi = 6.0 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
ChEMBL 233 4 0 2 2.9 CCN(CC)C1CCc2c(cccc2OC)C1 10.1021/jm960345l
25141538 63015 0 None -407 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627311 63015 0 None -407 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125]IABN from human D4 receptor expressed in HEK293 cellsDisplacement of [125]IABN from human D4 receptor expressed in HEK293 cells
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
681 8247 72 None -2 38 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 8247 72 None -2 38 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 8247 72 None -2 38 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 8247 72 None -2 38 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 8247 72 None -2 38 Human 7.0 pKi = 7.0 Binding
Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D4.4
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
44330694 114365 0 None 9 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 2 0 3 4.1 CCCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
CHEMBL318949 114365 0 None 9 2 Human 7.0 pKi = 7.0 Binding
Binding affinity to recombinant human dopamine receptor D4Binding affinity to recombinant human dopamine receptor D4
ChEMBL 260 2 0 3 4.1 CCCn1ncc2c1-c1c(C)sc(C)c1CCC2 10.1016/s0960-894x(03)00587-0
44403224 78690 0 None -10 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(F)n1 10.1016/j.bmcl.2005.07.037
CHEMBL197195 78690 0 None -10 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand Binding affinity towards Dopamine receptor D 4.4 using CHO cell line and [3H]spiperone as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(F)n1 10.1016/j.bmcl.2005.07.037
22100968 210883 4 None 2 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 290 3 0 3 4.1 C1=C(c2nc3ccccc3o2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
CHEMBL70267 210883 4 None 2 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cellsDisplacement of [3H]spiperone from human dopamine receptor subtype hD4 expressed in HEK293 cells
ChEMBL 290 3 0 3 4.1 C1=C(c2nc3ccccc3o2)CCN(Cc2ccccc2)C1 10.1016/S0960-894X(97)00402-2
11230330 141965 0 None -19 3 Human 5.0 pKi = 5.0 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
CHEMBL372020 141965 0 None -19 3 Human 5.0 pKi = 5.0 Binding
Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cellsLow inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
44415593 87022 0 None -977 6 Human 6.0 pKi = 6.0 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213834 87022 0 None -977 6 Human 6.0 pKi = 6.0 Binding
Binding affinity at dopamine D4 receptorBinding affinity at dopamine D4 receptor
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
154725234 183071 1 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4585289 183071 1 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4595149 183071 1 None -1 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
11547151 91140 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 10 1 7 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
CHEMBL221843 91140 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membraneDisplacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane
ChEMBL 462 10 1 7 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2nnn(Cc3ccccc3)c2C)CC1 10.1021/jm0611152
44275807 105746 0 None -8912 10 Human 5.0 pKi = 5.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
CHEMBL27979 105746 0 None -8912 10 Human 5.0 pKi = 5.0 Binding
Binding affinity towards human D4.2 receptorBinding affinity towards human D4.2 receptor
ChEMBL 422 7 0 4 4.5 C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1 10.1016/s0960-894x(03)00118-5
155515301 176746 0 None -812 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(C[C@H]2OCCOC2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2019.02.056
CHEMBL4441888 176746 0 None -812 7 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation countingDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 1 hr by liquid scintillation counting
ChEMBL 444 6 0 5 4.2 COc1ccccc1N1CCN(C[C@H]2OCCOC2(c2ccccc2)c2ccccc2)CC1 10.1016/j.ejmech.2019.02.056
49798874 21123 0 None -1096 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 488 7 0 7 3.8 O=C1N(Cc2cn(CCF)nn2)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1171630 21123 0 None -1096 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 488 7 0 7 3.8 O=C1N(Cc2cn(CCF)nn2)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
CHEMBL1200106 21123 0 None -1096 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma countingDisplacement of [125I]ABN from human dopamine D4 receptor expressed in HEK293 cells after 60 mins by gamma counting
ChEMBL 488 7 0 7 3.8 O=C1N(Cc2cn(CCF)nn2)CN(c2ccccc2)C12CCN(Cc1coc3ccccc13)CC2 10.1016/j.bmc.2010.05.052
122189391 130024 0 None -11 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613877 130024 0 None -11 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
16090814 88356 0 None -74 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 88356 0 None -74 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4 dopamine receptor expressed in CHO cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
142590731 189861 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 470 9 1 3 6.2 Fc1ccc(CN2CCC(NCCSC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2020.112674
CHEMBL4794406 189861 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by microbeta scintillation counting method
ChEMBL 470 9 1 3 6.2 Fc1ccc(CN2CCC(NCCSC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1016/j.ejmech.2020.112674
154704536 183226 1 None -1 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4467528 183226 1 None -1 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4596340 183226 1 None -1 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-N-methylspiperone from recombinant human D4 receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
11637457 79862 1 None -8 5 Human 7.0 pKi = 7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
CHEMBL201093 79862 1 None -8 5 Human 7.0 pKi = 7 Binding
Binding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assayBinding affinity to human cloned D4 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
51353678 66961 0 None -1905 3 Human 6.0 pKi = 6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 461 13 1 5 3.7 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(OCCF)cc1 10.1021/jm101323b
CHEMBL1689004 66961 0 None -1905 3 Human 6.0 pKi = 6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 461 13 1 5 3.7 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(OCCF)cc1 10.1021/jm101323b
CHEMBL1739810 66961 0 None -1905 3 Human 6.0 pKi = 6 Binding
Binding affinity to human D4 receptor transfected in human HEK293 cells by gamma-countingBinding affinity to human D4 receptor transfected in human HEK293 cells by gamma-counting
ChEMBL 461 13 1 5 3.7 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1ccc(OCCF)cc1 10.1021/jm101323b
44380921 65103 0 None -2 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168274 65103 0 None -2 4 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.Binding affinity towards human Dopamine receptor D4 by [3H]spiperone displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
11212939 75935 0 None 4 2 Rat 6.0 pKi = 6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
CHEMBL192439 75935 0 None 4 2 Rat 6.0 pKi = 6 Binding
Inhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membraneInhibition of [3H]spiperone binding to Dopamine receptor D2-like in rat caudate-putamen membrane
ChEMBL 443 7 1 4 4.5 COc1ccc2c(c1)N1CCN(CCCCNC(=O)c3ccc4ccccc4c3)C[C@@H]1CC2 10.1021/jm049031l
44336035 12066 0 None 2 2 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(Cl)cccc21 10.1016/s0960-894x(02)00655-8
CHEMBL106598 12066 0 None 2 2 Human 6.0 pKi = 6 Binding
Binding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligandBinding affinity towards human Dopamine Receptor D4 was determined via standard competitive displacement assays using [3H]-YM 09151 as radioligand
ChEMBL 403 4 0 3 3.7 O=C(CN1CCN(Cc2ccc(Cl)cc2)CC1)N1CCc2c(Cl)cccc21 10.1016/s0960-894x(02)00655-8
135 9310 43 None - 56 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 None - 56 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 None - 56 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 None - 56 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 None - 56 Human 8.3 pIC50 = 8.3 Binding
Binding affinity for human cloned Dopamine receptor D4Binding affinity for human cloned Dopamine receptor D4
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1353 8692 93 None -3 85 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 None -3 85 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 None -3 85 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 None -3 85 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 None -3 85 Human 8.0 pKd = 8.0 Binding
radioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cellsradioligand [3H]spiperone 0.5nM competition binding; human recombinant dopaminereceptors in CHO cells
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
9952220 105032 6 None -8 3 Human 8.0 pKd = 8.0 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
Drug Central 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)[C@H]2C)cc1Cl None
CHEMBL274491 105032 6 None -8 3 Human 8.0 pKd = 8.0 Binding
Binding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligandBinding Affinity to Human Dopamine receptor D4 expressed in CHO cells was determined using [3H]- nemonapride as radioligand
Drug Central 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)[C@H]2C)cc1Cl None
188942 9594 41 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
3297 9594 41 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
979 9594 41 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
CHEMBL103772 9594 41 None -12 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 9262371
2470 10425 50 None -20 58 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
2470 10425 50 None -20 58 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
3300 10425 50 None -20 58 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
3300 10425 50 None -20 58 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
5265 10425 50 None -20 58 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
5265 10425 50 None -20 58 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
99 10425 50 None -20 58 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
99 10425 50 None -20 58 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
CHEMBL267930 10425 50 None -20 58 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1840645
CHEMBL267930 10425 50 None -20 58 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7777184
4452 9538 19 None -7 18 Human 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 8248849
983 9538 19 None -7 18 Human 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 8248849
CHEMBL20734 9538 19 None -7 18 Human 10.0 pKd None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 8248849
4452 9538 19 3H-YM 09151-2 -7 18 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 9538 19 3H-YM 09151-2 -7 18 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 9538 19 3H-YM 09151-2 -7 18 Human 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
2470 10425 50 3H-SPIPERONE -4 58 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SPIPERONE -4 58 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SPIPERONE -4 58 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SPIPERONE -4 58 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SPIPERONE -4 58 Rat 10.3 pKi = 10.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
16363 7383 53 UNDEFINED -1 7 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
312 7383 53 UNDEFINED -1 7 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
9215 7383 53 UNDEFINED -1 7 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL297302 7383 53 UNDEFINED -1 7 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB12867 7383 53 UNDEFINED -1 7 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2470 10425 50 3H-SPIPERONE -20 58 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SPIPERONE -20 58 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SPIPERONE -20 58 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SPIPERONE -20 58 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SPIPERONE -20 58 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 10425 50 3H-SPIPERONE -20 58 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SPIPERONE -20 58 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SPIPERONE -20 58 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SPIPERONE -20 58 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SPIPERONE -20 58 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
None 223057 0 UNDEFINED 4 12 Human 10.1 pKi = 10.1 Binding
NoneNone
PDSP KiDatabase 426 6 0 6 3.4 C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54 None
2 10035 23 3H-SPIPERONE -2 28 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 10035 23 3H-SPIPERONE -2 28 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 10035 23 3H-SPIPERONE -2 28 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
2389 10104 118 3H-SPIPERONE -22 66 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 10104 118 UNDEFINED -22 66 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SPIPERONE -22 66 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 UNDEFINED -22 66 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SPIPERONE -22 66 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 UNDEFINED -22 66 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SPIPERONE -22 66 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 UNDEFINED -22 66 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SPIPERONE -22 66 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 UNDEFINED -22 66 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1353 8692 93 3H-SPIPERONE -3 85 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SPIPERONE -3 85 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SPIPERONE -3 85 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SPIPERONE -3 85 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SPIPERONE -3 85 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
5567 49576 27 UNDEFINED -11 8 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 49576 27 UNDEFINED -11 8 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
2470 10425 50 3H-SPIPERONE -4 58 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SPIPERONE -4 58 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SPIPERONE -4 58 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SPIPERONE -4 58 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SPIPERONE -4 58 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1238 209953 24 R-SAT -2 16 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 209953 24 R-SAT -2 16 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
3303 9024 46 UNDEFINED 1 15 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
5311200 9024 46 UNDEFINED 1 15 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
CHEMBL267014 9024 46 UNDEFINED 1 15 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
11976 7707 59 UNDEFINED -2 24 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 7707 59 UNDEFINED -2 24 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 7707 59 UNDEFINED -2 24 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 7707 59 UNDEFINED -2 24 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1353 8692 93 3H-SPIROPERIDOL -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SPIROPERIDOL -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SPIROPERIDOL -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SPIROPERIDOL -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SPIROPERIDOL -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2865 10915 73 UNDEFINED -66 53 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 UNDEFINED -66 53 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 UNDEFINED -66 53 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 UNDEFINED -66 53 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 UNDEFINED -66 53 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1353 8692 93 3H-Haloperidol -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 3H-SPIPERONE -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 UNDEFINED -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-Haloperidol -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SPIPERONE -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 UNDEFINED -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-Haloperidol -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SPIPERONE -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 UNDEFINED -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-Haloperidol -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SPIPERONE -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 UNDEFINED -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-Haloperidol -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SPIPERONE -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 UNDEFINED -3 85 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3168 16034 92 UNDEFINED -4 22 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 16034 92 UNDEFINED -4 22 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
2435 10362 83 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-SPIPERONE -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 10362 83 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 UNDEFINED -10 48 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2435 10362 83 3H-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-Sertindole -10 48 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2726 7706 68 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SPIPERONE -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 7706 68 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 7706 68 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-Chlorpromazine -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 UNDEFINED -8 72 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2470 10425 50 3H-SPIPERONE -20 58 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SPIPERONE -20 58 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SPIPERONE -20 58 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SPIPERONE -20 58 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SPIPERONE -20 58 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
100 10577 58 3H-SPIPERONE -8 54 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
100 10577 58 UNDEFINED -8 54 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-SPIPERONE -8 54 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 UNDEFINED -8 54 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-SPIPERONE -8 54 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 UNDEFINED -8 54 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-SPIPERONE -8 54 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 UNDEFINED -8 54 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-SPIPERONE -8 54 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 UNDEFINED -8 54 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
135398737 7745 93 3H-Clozapine -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 3H-SPIPERONE -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 UNDEFINED -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-Clozapine -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIPERONE -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 UNDEFINED -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-Clozapine -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIPERONE -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 UNDEFINED -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-Clozapine -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIPERONE -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 UNDEFINED -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-Clozapine -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIPERONE -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 UNDEFINED -13 90 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5281878 8441 35 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 UNDEFINED -14 16 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 9688 112 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 9688 112 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-Olanzapine -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 UNDEFINED -10 65 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3303 9024 46 R-SAT 1 15 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
5311200 9024 46 R-SAT 1 15 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
CHEMBL267014 9024 46 R-SAT 1 15 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 None
16362 9899 71 R-SAT -20 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 R-SAT -20 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 R-SAT -20 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 R-SAT -20 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 R-SAT -20 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
46780481 114308 20 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-NMSP -23 53 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1613 9127 53 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-NEMONAPRIDE -2 44 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
100 10577 58 3H-SPIPERONE -3 54 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-SPIPERONE -3 54 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-SPIPERONE -3 54 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-SPIPERONE -3 54 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-SPIPERONE -3 54 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
115368 9830 47 None 1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
2112 9830 47 None 1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
7556 9830 47 None 1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
CHEMBL1472975 9830 47 None 1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
DB08922 9830 47 None 1 4 Human 8.0 pKi = 8 Binding
NoneNone
Drug Central 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 None
2435 10362 83 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-SPIPERONE -19 48 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1353 8692 93 3H-SPIPERONE -4 85 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SPIPERONE -4 85 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SPIPERONE -4 85 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SPIPERONE -4 85 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SPIPERONE -4 85 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
100 10577 58 3H-SPIPERONE -8 54 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-SPIPERONE -8 54 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-SPIPERONE -8 54 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-SPIPERONE -8 54 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-SPIPERONE -8 54 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
4257 85030 30 None - 1 Human 8.0 pKi = 8.0 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
Drug Central 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 None
CHEMBL2106650 85030 30 None - 1 Human 8.0 pKi = 8.0 Binding
Agonist activity at dopamine D4 receptor (unknown origin)Agonist activity at dopamine D4 receptor (unknown origin)
Drug Central 478 4 1 4 4.7 O=C1NC2CCCCN2C12CCN(CCCN1c3ccccc3CCc3ccc(Cl)cc31)CC2 None
25139335 191097 0 UNDEFINED 2 3 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 None
CHEMBL484203 191097 0 UNDEFINED 2 3 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 314 8 0 4 3.6 CC#CC1=CCC(N(CCC)CCCCn2cc(C)nn2)CC1 None
242 7258 124 R-SAT -104 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 R-SAT -104 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 R-SAT -104 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 R-SAT -104 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 R-SAT -104 51 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
5281878 8441 35 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 R-SAT -14 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2865 10915 73 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 R-SAT -66 53 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
15387 52596 55 R-SAT -35 24 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 52596 55 R-SAT -35 24 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
54477 91428 36 R-SAT -14 22 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 91428 36 R-SAT -14 22 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
164512405 222728 0 3H-SPIPERONE -10 12 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
119192 9259 54 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
1582 9259 54 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
CHEMBL506981 9259 54 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
DB06455 9259 54 3H-N-Methylspiporone -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
134 9292 24 3H-NMSP -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-NMSP -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-NMSP -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-NMSP -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-NMSP -8511 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
15897 9637 0 3H-NMSP -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-NMSP -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-NMSP -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
128563 10237 33 3H-NMSP -2398 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 10237 33 3H-NMSP -2398 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 10237 33 3H-NMSP -2398 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 10237 33 3H-NMSP -2398 42 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
189 10265 39 3H-YM 09151-1 -4168 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
5163 10265 39 3H-YM 09151-1 -4168 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
CHEMBL297784 10265 39 3H-YM 09151-1 -4168 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 1 1 3 3.2 O=C(N1CCc2c1cc1ccn(c1c2)C)Nc1cccnc1 None
185 10778 60 3H-NMSP -7244 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 10778 60 3H-NMSP -7244 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 10778 60 3H-NMSP -7244 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 10778 60 3H-NMSP -7244 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
2662 18156 131 3H-NMSP -41 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 18156 131 3H-NMSP -41 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
10297 33885 30 3H-NMSP -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 33885 30 3H-NMSP -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
156391 53574 99 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 53574 99 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 53574 99 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
10624 77075 19 3H-NMSP -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 77075 19 3H-NMSP -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 77075 19 3H-NMSP -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
2244 101008 100 3H-NMSP -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 101008 100 3H-NMSP -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
24840389 121991 4 3H-SPIPERONE -7413 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
CHEMBL334529 121991 4 3H-SPIPERONE -7413 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
446220 140299 14 3H-NMSP -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 140299 14 3H-NMSP -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
1615 174570 24 3H-NMSP -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
1615 174570 24 3H-NMSP -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 174570 24 3H-NMSP -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 174570 24 3H-NMSP -26 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
3672 199312 136 3H-NMSP -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
CHEMBL521 199312 136 3H-NMSP -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
54676228 200394 112 3H-NMSP -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 200394 112 3H-NMSP -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
4495 203314 92 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 203314 92 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 207330 115 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 207330 115 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 207330 115 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 209053 22 3H-NMSP -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 3H-NMSP -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 3H-NMSP -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
5281600 209804 92 3H-Methylspiperone -275 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 209804 92 3H-Methylspiperone -275 32 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
3821 211497 17 3H-N-Methylspiperone -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
CHEMBL742 211497 17 3H-N-Methylspiperone -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
4054 212280 72 3H-NMSP -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 212280 72 3H-NMSP -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 212280 72 3H-NMSP -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
3337 213146 27 3H-NMSP -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 3H-NMSP -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 3H-NMSP -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 3H-NMSP -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 3H-NMSP -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
164512405 222728 0 3H-SPIPERONE -33 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
11954224 222732 0 3H-NMSP -141253 59 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
None 222772 0 3H-N-Methylspiperone -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
25137849 222958 0 3H-NMSP -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 222958 0 3H-NMSP -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
None 223018 0 3H-NMSP -95499 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 223090 0 3H-NMSP -1 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 223091 0 3H-NMSP -1 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 223092 0 3H-NMSP -1 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 223093 0 3H-NMSP -1 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 223094 0 3H-NMSP -1 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 223095 0 3H-NMSP -1 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 223096 0 3H-NMSP -1 39 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 223097 0 3H-NMSP -1 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 223104 0 3H-NMSP -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 223105 0 3H-NMSP -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 223106 0 3H-Methylspiperone -16 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
None 223108 0 3H-Methylspiperone -3 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 223109 0 3H-Methylspiperone -281 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 223110 0 3H-Methylspiperone -1 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
135269 223168 0 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 223169 0 3H-NMSP -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 223170 0 3H-NMSP -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
84003 223171 0 3H-NMSP -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
119828 223173 0 3H-NMSP -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 223229 0 3H-SPIPERONE -660 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 223229 0 UNDEFINED -660 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 223268 0 3H-NMSP -4570 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
164512405 222728 0 3H-SPIPERONE -10 12 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
135409468 8816 69 3H-NMSP -18 39 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 8816 69 3H-NMSP -18 39 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 8816 69 3H-NMSP -18 39 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
44395711 181678 0 UNDEFINED -5 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 None
CHEMBL456430 181678 0 UNDEFINED -5 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 None
CHEMBL537183 181678 0 UNDEFINED -5 3 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 345 3 1 2 4.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1ccc(F)cc1 None
1353 8692 93 UNDEFINED -3 85 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 UNDEFINED -3 85 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 UNDEFINED -3 85 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 UNDEFINED -3 85 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 UNDEFINED -3 85 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2865 10915 73 3H-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-NMSP -66 53 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2337 10030 77 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SPIPERONE -114 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
9906978 49485 2 UNDEFINED 1 12 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 49485 2 UNDEFINED 1 12 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
25139329 193882 0 UNDEFINED -7 4 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 None
CHEMBL491466 193882 0 UNDEFINED -7 4 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 None
2274 9947 58 R-SAT -56 31 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 R-SAT -56 31 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 R-SAT -56 31 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 R-SAT -56 31 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 R-SAT -56 31 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2337 10030 77 3H-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SPIPERONE -173 62 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
37459 7533 13 3H-SPIPERONE -123 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SPIPERONE -123 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SPIPERONE -123 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
1613 9127 53 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1613 9127 53 3H-SPIPERONE -3 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-SPIPERONE -3 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-SPIPERONE -3 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-SPIPERONE -3 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-NMSP -2 44 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-SPIPERONE -3 44 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
100 10577 58 3H-SPIPERONE -3 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-SPIPERONE -3 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-SPIPERONE -3 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-SPIPERONE -3 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-SPIPERONE -3 54 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2726 7706 68 3H-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SPIPERONE -10 72 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1353 8692 93 UNDEFINED -3 85 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 UNDEFINED -3 85 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 UNDEFINED -3 85 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 UNDEFINED -3 85 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 UNDEFINED -3 85 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
277 8083 62 3H-Methylspiperone -144 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 3H-Methylspiperone -144 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 3H-Methylspiperone -144 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 3H-Methylspiperone -144 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 3H-Methylspiperone -144 50 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
None 223008 0 3H-YM 09151-2 15 2 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 291 3 2 2 3.8 C1=CC=C2C(=C1)C=CC=C2NC(=O)C3=CC=CC=C3C(=O)O None
2337 10030 77 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-NMSP -114 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
44591089 196261 0 UNDEFINED - 1 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 None
CHEMBL513776 196261 0 UNDEFINED - 1 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 327 3 2 3 3.3 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ncccc23)C1 None
2 10035 23 3H-SPIPERONE -2 28 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 10035 23 3H-SPIPERONE -2 28 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 10035 23 3H-SPIPERONE -2 28 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
4978 223107 0 3H-Methylspiperone 7 27 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
119570 9933 96 3H-SPIPERONE -6 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 3H-SPIPERONE -6 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 3H-SPIPERONE -6 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 3H-SPIPERONE -6 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 3H-SPIPERONE -6 39 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
6603820 102549 19 3H-SCH23390 -1 12 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 102549 19 3H-SCH23390 -1 12 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
None 223008 0 3H-SPIPERONE 15 2 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 291 3 2 2 3.8 C1=CC=C2C(=C1)C=CC=C2NC(=O)C3=CC=CC=C3C(=O)O None
1712 9270 43 3H-SPIPERONE -3 22 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 9270 43 3H-SPIPERONE -3 22 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 9270 43 3H-SPIPERONE -3 22 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 9270 43 3H-SPIPERONE -3 22 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 9270 43 3H-SPIPERONE -3 22 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
101 10594 24 3H-SPIPERONE -54 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
55752 10594 24 3H-SPIPERONE -54 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL35057 10594 24 3H-SPIPERONE -54 14 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 6 0 6 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1nsc2c1cccc2 None
279 8442 26 3H-SPIPERONE -26 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 8442 26 3H-SPIPERONE -26 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 8442 26 3H-SPIPERONE -26 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
5281878 8441 35 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 R-SAT -14 16 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 222939 0 3H-YM 09151-2 -1 3 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 233 4 1 2 3.1 CCCNC1CCC2=C(C1C)C=CC=C2OC None
3033769 10054 61 3H-YM 09151-2 -562 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 3H-YM 09151-2 -562 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 3H-YM 09151-2 -562 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 3H-YM 09151-2 -562 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 3H-YM 09151-2 -562 18 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
15387 52596 55 3H-YM 09151-2 -35 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 52596 55 3H-YM 09151-2 -35 24 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
135398745 9688 112 3H-SPIPERONE -10 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SPIPERONE -10 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SPIPERONE -10 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SPIPERONE -10 65 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5467 212707 43 R-SAT 6 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
CHEMBL84158 212707 43 R-SAT 6 5 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
2274 9947 58 3H-NEMONAPRIDE -56 31 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 3H-NEMONAPRIDE -56 31 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 3H-NEMONAPRIDE -56 31 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 3H-NEMONAPRIDE -56 31 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 3H-NEMONAPRIDE -56 31 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
25139332 191098 0 UNDEFINED -1 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
CHEMBL484204 191098 0 UNDEFINED -1 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
None 224136 0 UNDEFINED -380 4 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 451 3 0 7 3.9 CC1=NC2=C(C=C1)C3=C(C=C2)OCC(O3)CN4CCN(CC4)C5=NC6=C(C=C5)C=C(C=C6)C#N None
3663 106743 83 3H-Methylspiperone -42 28 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 106743 83 3H-Methylspiperone -42 28 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
1353 8692 93 3H-NMSP -3 85 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-NMSP -3 85 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-NMSP -3 85 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-NMSP -3 85 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-NMSP -3 85 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 9688 112 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SPIPERONE -7 65 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2726 7706 68 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-YM 09151-2 -8 72 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
133633 9021 53 UNDEFINED -104 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 None
177 9021 53 UNDEFINED -104 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 None
CHEMBL445102 9021 53 UNDEFINED -104 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 None
2435 10362 83 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-NEMONAPRIDE -10 48 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
104911 222798 0 3H-NMSP -67 37 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
2389 10104 118 3H-SPIPERONE -30 66 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SPIPERONE -30 66 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SPIPERONE -30 66 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SPIPERONE -30 66 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SPIPERONE -30 66 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2337 10030 77 3H-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-NEMONAPRIDE -114 62 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
6852400 222716 0 R-SAT -794 22 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 222716 0 R-SAT -794 22 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
209 9831 97 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 9831 97 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 9831 97 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 9831 97 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 9831 97 UNDEFINED -30 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
100 10577 58 3H-NMSP -8 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-NMSP -8 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-NMSP -8 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-NMSP -8 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-NMSP -8 54 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
44395741 188360 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476935 188360 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL558392 188360 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
44395741 188360 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476935 188360 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL558392 188360 0 UNDEFINED 1 10 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
44350664 124927 0 UNDEFINED -1 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL340816 124927 0 UNDEFINED -1 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL553417 124927 0 UNDEFINED -1 6 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 351 6 0 2 5.2 O=C(CCCN1C2CCC1CC(c1ccccc1)C2)c1ccc(F)cc1 None
2389 10104 118 3H-NEMONAPRIDE -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 10104 118 R-SAT -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-NEMONAPRIDE -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 R-SAT -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-NEMONAPRIDE -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 R-SAT -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-NEMONAPRIDE -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 R-SAT -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-NEMONAPRIDE -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 R-SAT -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
103 10925 61 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-NMSP -17 53 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2389 10104 118 3H-NMSP -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-NMSP -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-NMSP -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-NMSP -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-NMSP -22 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
44591045 183516 0 UNDEFINED 19 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 None
CHEMBL460223 183516 0 UNDEFINED 19 3 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 3 1 3 3.9 Clc1ccc(N2CCCN(Cc3c[nH]c4ncccc34)CC2)cc1 None
25139478 191735 0 UNDEFINED -138 4 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 None
CHEMBL485384 191735 0 UNDEFINED -138 4 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 None
135398745 9688 112 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-NMSP -10 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
214 10632 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 10632 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 10632 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 10632 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 10632 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 10632 58 3H-SPIPERONE -22 30 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 223121 0 3H-SPIPERONE -3 19 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
13091273 189217 0 UNDEFINED -8 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL478617 189217 0 UNDEFINED -8 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
CHEMBL553327 189217 0 UNDEFINED -8 6 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 367 6 1 3 4.3 O=C(CCCN1C2CCC1CC(O)(c1ccccc1)C2)c1ccc(F)cc1 None
25139479 191096 0 UNDEFINED -21 4 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 None
CHEMBL484202 191096 0 UNDEFINED -21 4 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 None
191 7191 98 UNDEFINED -8 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 7191 98 UNDEFINED -8 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 7191 98 UNDEFINED -8 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 7191 98 UNDEFINED -8 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 7191 98 UNDEFINED -8 29 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
1353 8692 93 3H-SPIPERONE -3 85 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SPIPERONE -3 85 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SPIPERONE -3 85 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SPIPERONE -3 85 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SPIPERONE -3 85 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 9688 112 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SPIPERONE -10 65 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
4249 84954 34 UNDEFINED -7 6 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 84954 34 UNDEFINED -7 6 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
1353 8692 93 3H-SPIPERONE -4 85 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SPIPERONE -4 85 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SPIPERONE -4 85 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SPIPERONE -4 85 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SPIPERONE -4 85 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3294 8787 111 UNDEFINED -11 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 UNDEFINED -11 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 UNDEFINED -11 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 UNDEFINED -11 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 UNDEFINED -11 44 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
1353 8692 93 3H-NEMONAPRIDE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 3H-YM 09151-2 -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-NEMONAPRIDE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-YM 09151-2 -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-NEMONAPRIDE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-YM 09151-2 -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-NEMONAPRIDE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-YM 09151-2 -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-NEMONAPRIDE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-YM 09151-2 -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2726 7706 68 3H-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SCH23390 -10 72 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135409468 8816 69 UNDEFINED -18 39 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 8816 69 UNDEFINED -18 39 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 8816 69 UNDEFINED -18 39 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
164512405 222728 0 3H-SPIPERONE -10 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
None 222792 0 3H-SPIPERONE -7 3 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 310 3 0 2 4.8 CN(C)CCC=C1C2=CC=CC=C2C=NC3=C1C=C(C=C3)Cl None
164512405 222728 0 UNDEFINED -10 12 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
2337 10030 77 3H-SPIPERONE -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 10030 77 3H-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SPIPERONE -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SPIPERONE -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SPIPERONE -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SPIPERONE -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SPIPERONE -173 62 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
164512405 222728 0 3H-NEMONAPRIDE -10 12 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
11954259 222758 0 3H-NMSP -676 43 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
135398737 7745 93 3H-SPIPERONE -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 3H-SPIROPERIDOL -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIPERONE -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIROPERIDOL -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIPERONE -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIROPERIDOL -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIPERONE -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIROPERIDOL -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIPERONE -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIROPERIDOL -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
279 8442 26 UNDEFINED -4 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 8442 26 UNDEFINED -4 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 8442 26 UNDEFINED -4 17 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
164512405 222728 0 3H-SPIPERONE -10 12 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
21830793 98610 10 3H-8-OH-DPAT -144 46 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 98610 10 3H-8-OH-DPAT -144 46 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
44578445 188358 0 UNDEFINED -13 3 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 None
CHEMBL476933 188358 0 UNDEFINED -13 3 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 352 6 0 3 4.1 O=C(CCCN1CC2CCC(C1)N2c1ccccc1)c1ccc(F)cc1 None
135398737 7745 93 3H-SPIPERONE -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 7745 93 3H-SPIPERONE -7 90 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIPERONE -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIPERONE -7 90 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIPERONE -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIPERONE -7 90 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIPERONE -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIPERONE -7 90 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIPERONE -13 90 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIPERONE -7 90 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1353 8692 93 R-SAT -3 85 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 R-SAT -3 85 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 R-SAT -3 85 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 R-SAT -3 85 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 R-SAT -3 85 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
44134711 222770 0 3H-SPIPERONE -275 13 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
100 10577 58 3H-YM 09151-2 -8 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-YM 09151-2 -8 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-YM 09151-2 -8 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-YM 09151-2 -8 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-YM 09151-2 -8 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2337 10030 77 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 UNDEFINED -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
54477 91428 36 3H-NEMONAPRIDE -14 22 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 91428 36 3H-NEMONAPRIDE -14 22 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
2337 10030 77 3H-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-N-Methylspiperone -114 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
None 223399 0 UNDEFINED -102 3 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 453 10 0 7 4.2 CCOC1=CC=CC=C1N2CCN(CC2)CCCC3CC(=NO3)C4=CC(=C(C=C4)OC)OC None
2726 7706 68 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-NEMONAPRIDE -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1212 8443 50 3H-NEMONAPRIDE -77 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-NEMONAPRIDE -77 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-NEMONAPRIDE -77 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-NEMONAPRIDE -77 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-NEMONAPRIDE -77 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
65750 223225 0 R-SAT -1 3 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 346 6 0 3 5.7 CCN(CC)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl None
15387 52596 55 3H-SPIPERONE -33 24 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 52596 55 3H-SPIPERONE -33 24 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
243 9976 91 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 9976 91 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 9976 91 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 9976 91 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 9976 91 3H-SPIPERONE -12 34 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
179 7188 115 3H-NMSP -50 50 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 3H-NMSP -50 50 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 3H-NMSP -50 50 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 3H-NMSP -50 50 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 3H-NMSP -50 50 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
3033769 10054 61 3H-SPIPERONE -288 18 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 3H-SPIPERONE -288 18 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 3H-SPIPERONE -288 18 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 3H-SPIPERONE -288 18 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 3H-SPIPERONE -288 18 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
2726 7706 68 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 7706 68 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-NMSP -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 R-SAT -8 72 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1830 9368 44 3H-SPIPERONE -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 9368 44 UNDEFINED -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 3H-SPIPERONE -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 UNDEFINED -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 3H-SPIPERONE -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 UNDEFINED -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 3H-SPIPERONE -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 UNDEFINED -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 3H-SPIPERONE -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 UNDEFINED -120 28 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
3033769 10054 61 3H-SPIPERONE -562 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 10054 61 3H-SPIPERONE -288 18 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 3H-SPIPERONE -562 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 3H-SPIPERONE -288 18 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 3H-SPIPERONE -562 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 3H-SPIPERONE -288 18 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 3H-SPIPERONE -562 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 3H-SPIPERONE -288 18 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 3H-SPIPERONE -562 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 3H-SPIPERONE -288 18 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
54477 91428 36 3H-SPIPERONE -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 91428 36 3H-SPIPERONE -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
9906978 49485 2 UNDEFINED 1 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 49485 2 UNDEFINED 1 12 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
3294 8787 111 3H-SPIPERONE -11 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-SPIPERONE -11 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-SPIPERONE -11 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-SPIPERONE -11 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-SPIPERONE -11 44 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
100 10577 58 3H-NEMONAPRIDE -8 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-NEMONAPRIDE -8 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-NEMONAPRIDE -8 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-NEMONAPRIDE -8 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-NEMONAPRIDE -8 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
242 7258 124 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-Methylspiperone -87 51 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
135398745 9688 112 3H-SPIPERONE -10 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SPIPERONE -10 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SPIPERONE -10 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SPIPERONE -10 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
4249 84954 34 R-SAT -7 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 84954 34 R-SAT -7 6 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
44134711 222770 0 3H-SPIPERONE -275 13 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
44591042 183590 0 UNDEFINED -15 3 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 None
CHEMBL460854 183590 0 UNDEFINED -15 3 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 380 4 2 2 4.9 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCc1c[nH]c2ccccc12 None
2435 10362 83 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 R-SAT -10 48 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
135398737 7745 93 3H-YM 09151-2 -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-YM 09151-2 -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-YM 09151-2 -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-YM 09151-2 -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-YM 09151-2 -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
163839 9729 0 3H-Methylspiperone -15 6 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
268 9729 0 3H-Methylspiperone -15 6 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
CHEMBL55171 9729 0 3H-Methylspiperone -15 6 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
54477 91428 36 3H-SPIPERONE -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
54477 91428 36 UNDEFINED -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
54477 91428 36 3H-SPIPERONE -38 22 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 91428 36 3H-SPIPERONE -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 91428 36 UNDEFINED -14 22 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 91428 36 3H-SPIPERONE -38 22 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
31101 7516 40 3H-SPIPERONE -186 35 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 3H-SPIPERONE -186 35 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 3H-SPIPERONE -186 35 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 3H-SPIPERONE -186 35 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 3H-SPIPERONE -186 35 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
135398737 7745 93 3H-Methylspiperone -7 90 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-Methylspiperone -7 90 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-Methylspiperone -7 90 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-Methylspiperone -7 90 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-Methylspiperone -7 90 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 9127 53 3H-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-YM 09151-2 -2 44 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
119570 9933 96 3H-NMSP -6 39 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 3H-NMSP -6 39 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 3H-NMSP -6 39 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 3H-NMSP -6 39 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 3H-NMSP -6 39 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
135398745 9688 112 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SCH23390 -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3033769 10054 61 3H-SPIPERONE -562 18 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 3H-SPIPERONE -562 18 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 3H-SPIPERONE -562 18 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 3H-SPIPERONE -562 18 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 3H-SPIPERONE -562 18 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
1353 8692 93 3H-SPIPERONE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SPIPERONE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SPIPERONE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SPIPERONE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SPIPERONE -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 UNDEFINED -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 UNDEFINED -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 UNDEFINED -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 UNDEFINED -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 UNDEFINED -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 3H-N-Methylspiperone -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-N-Methylspiperone -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-N-Methylspiperone -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-N-Methylspiperone -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-N-Methylspiperone -3 85 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 223009 0 3H-YM 09151-2 -3 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 359 1 2 2 3.7 CC(C)(C)C(=O)NC1CC2C(CC3=C(NC4=CC=CC2=C34)Cl)N(C1)C None
3691783 11536 1 UNDEFINED 47 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 None
CHEMBL103871 11536 1 UNDEFINED 47 3 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 3.4 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)c[nH]2)cc1 None
CHEMBL146246 45052 0 3H-SPIPERONE -1 9 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 401 5 1 5 2.2 NS(=O)(=O)c1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 None
9906978 49485 2 UNDEFINED 1 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
CHEMBL150161 49485 2 UNDEFINED 1 12 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 6 1 3 4.0 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)C1)c1ccc(F)cc1 None
2470 10425 50 R-SAT -20 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 R-SAT -20 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 R-SAT -20 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 R-SAT -20 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 R-SAT -20 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
100 10577 58 3H-SPIPERONE -3 54 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-SPIPERONE -3 54 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-SPIPERONE -3 54 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-SPIPERONE -3 54 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-SPIPERONE -3 54 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
135398737 7745 93 3H-SPIROPERIDOL -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIROPERIDOL -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIROPERIDOL -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIROPERIDOL -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIROPERIDOL -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1212 8443 50 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-SPIPERONE -77 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 9688 112 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-NEMONAPRIDE -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
16362 9899 71 3H-SPIPERONE -186 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-SPIPERONE -186 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-SPIPERONE -186 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-SPIPERONE -186 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-SPIPERONE -186 29 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
5074 10105 80 UNDEFINED -52 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 10105 80 UNDEFINED -52 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 10105 80 UNDEFINED -52 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 10105 80 UNDEFINED -52 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
16106 124924 34 3H-SPIPERONE -1 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
16106 124924 34 UNDEFINED -1 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 124924 34 3H-SPIPERONE -1 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 124924 34 UNDEFINED -1 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
None 223194 0 3H-SPIPERONE -97 5 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 453 8 1 4 4.6 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4C=C3.Cl None
2337 10030 77 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2337 10030 77 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-SPIPERONE -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 UNDEFINED -114 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
None 223942 0 UNDEFINED -120 3 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 366 3 2 2 4.8 C1CC2CC(CC1N2CC3=CNC4=CC=CC=C43)(C5=CC=C(C=C5)Cl)O None
2202 9906 96 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 9906 96 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 9906 96 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 9906 96 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 9906 96 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
135398745 9688 112 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 R-SAT -10 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
33630 185736 99 3H-SPIPERONE -5 28 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 185736 99 3H-SPIPERONE -5 28 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
25139180 191120 0 UNDEFINED -10 4 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 None
CHEMBL484357 191120 0 UNDEFINED -10 4 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 None
135398737 7745 93 3H-SPIPERONE -7 90 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIPERONE -7 90 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIPERONE -7 90 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIPERONE -7 90 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIPERONE -7 90 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
209 9831 97 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 9831 97 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 9831 97 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 9831 97 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 9831 97 3H-SPIPERONE -30 23 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2865 10915 73 UNDEFINED -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 UNDEFINED -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 UNDEFINED -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 UNDEFINED -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 UNDEFINED -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
214 10632 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 10632 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 10632 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 10632 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 10632 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 10632 58 3H-YM 09151-2 -33 30 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2865 10915 73 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-N-Methylspiperone -66 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
5567 49576 27 R-SAT -11 8 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 49576 27 R-SAT -11 8 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
2 10035 23 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 10035 23 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 10035 23 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
104870 105656 47 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 105656 47 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 105656 47 3H-SPIPERONE -2 21 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
2 10035 23 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 10035 23 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 10035 23 3H-SPIPERONE -2 28 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
135398737 7745 93 3H-SPIPERONE -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIPERONE -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIPERONE -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIPERONE -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIPERONE -13 90 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
31101 7516 40 3H-SPIPERONE -489 35 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 3H-SPIPERONE -489 35 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 3H-SPIPERONE -489 35 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 3H-SPIPERONE -489 35 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 3H-SPIPERONE -489 35 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
1830 9368 44 3H-SPIPERONE -120 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 3H-SPIPERONE -120 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 3H-SPIPERONE -120 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 3H-SPIPERONE -120 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 3H-SPIPERONE -120 28 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
3036864 209533 19 3H-SPIPERONE -14791 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 3H-SPIPERONE -14791 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 3H-SPIPERONE -14791 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 3H-SPIPERONE -14791 27 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
1212 8443 50 3H-NMSP -77 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-NMSP -77 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-NMSP -77 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-NMSP -77 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-NMSP -77 65 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
54477 91428 36 3H-SPIPERONE -14 22 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 91428 36 3H-SPIPERONE -14 22 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
2726 7706 68 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SPIPERONE -10 72 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
31101 7516 40 3H-SPIPERONE -186 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 3H-SPIPERONE -186 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 3H-SPIPERONE -186 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 3H-SPIPERONE -186 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 3H-SPIPERONE -186 35 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
6917970 10463 61 3H-NMSP -851 33 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 10463 61 3H-NMSP -851 33 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 10463 61 3H-NMSP -851 33 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
37459 7533 13 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
135398737 7745 93 3H-NMSP -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-NMSP -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-NMSP -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-NMSP -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-NMSP -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
214 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 223194 0 3H-SPIPERONE -97 5 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 453 8 1 4 4.6 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4C=C3.Cl None
None 223011 0 3H-SPIPERONE 1 4 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 226 0 2 2 1.4 C1CCC(=O)NCCCCCC(=O)NCC1 None
186 8588 52 3H-NMSP -645 17 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 8588 52 3H-NMSP -645 17 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 8588 52 3H-NMSP -645 17 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
30137 9652 0 3H-SPIPERONE -10 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 9652 0 3H-SPIPERONE -10 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 9652 0 3H-SPIPERONE -10 9 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
2470 10425 50 3H-SPIPERONE -20 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-SPIPERONE -20 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-SPIPERONE -20 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-SPIPERONE -20 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-SPIPERONE -20 58 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
25139181 191121 0 UNDEFINED -2 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 None
CHEMBL484358 191121 0 UNDEFINED -2 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 None
25058166 222739 0 3H-SPIPERONE -8 26 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-SPIPERONE -8 26 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
2389 10104 118 3H-SPIPERONE -22 66 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SPIPERONE -22 66 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SPIPERONE -22 66 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SPIPERONE -22 66 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SPIPERONE -22 66 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
37459 7533 13 UNDEFINED -123 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 UNDEFINED -123 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 UNDEFINED -123 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
71240 214496 14 R-SAT -9 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 408 4 1 3 4.0 OCCN1CCN([C@@H]2C[C@@H](c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 None
CHEMBL95636 214496 14 R-SAT -9 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 408 4 1 3 4.0 OCCN1CCN([C@@H]2C[C@@H](c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 None
1588 9105 27 3H-SPIPERONE -16 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 3H-SPIPERONE -16 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 3H-SPIPERONE -16 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 3H-SPIPERONE -16 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 3H-SPIPERONE -16 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1613 9127 53 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-SPIROPERIDOL -2 44 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
191 7191 98 R-SAT -8 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 7191 98 R-SAT -8 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 7191 98 R-SAT -8 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 7191 98 R-SAT -8 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 7191 98 R-SAT -8 29 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
37459 7533 13 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SPIPERONE -123 24 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
135398737 7745 93 3H-NEMONAPRIDE -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-NEMONAPRIDE -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-NEMONAPRIDE -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-NEMONAPRIDE -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-NEMONAPRIDE -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
214 10632 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 10632 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 10632 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 10632 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 10632 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 10632 58 3H-NEMONAPRIDE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398737 7745 93 3H-SPIPERONE -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIPERONE -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIPERONE -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIPERONE -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIPERONE -13 90 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11545813 187973 0 UNDEFINED 4 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 None
CHEMBL476109 187973 0 UNDEFINED 4 7 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 400 6 0 3 5.2 O=C(CCCN1C2CCC1CN(c1ccc(Cl)cc1)CC2)c1ccc(F)cc1 None
15387 52596 55 3H-SPIPERONE -35 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
15387 52596 55 UNDEFINED -35 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 52596 55 3H-SPIPERONE -35 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 52596 55 UNDEFINED -35 24 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
3033769 10054 61 3H-NEMONAPRIDE -562 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 3H-NEMONAPRIDE -562 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 3H-NEMONAPRIDE -562 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 3H-NEMONAPRIDE -562 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 3H-NEMONAPRIDE -562 18 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
25058166 222739 0 3H-SPIPERONE -8 26 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-SPIPERONE -8 26 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
None 223398 0 UNDEFINED -69 3 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 535 10 0 6 5.7 COC1=C(C=C(C=C1)C2=NOC(C2)CCCN3CCN(CC3)C(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)OC None
16362 9899 71 3H-SPIPERONE -186 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 3H-SPIPERONE -186 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 3H-SPIPERONE -186 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 3H-SPIPERONE -186 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 3H-SPIPERONE -186 29 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
1830 9368 44 3H-NEMONAPRIDE -120 28 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 3H-NEMONAPRIDE -120 28 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 3H-NEMONAPRIDE -120 28 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 3H-NEMONAPRIDE -120 28 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 3H-NEMONAPRIDE -120 28 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
214 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
214 10632 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 10632 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 10632 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 10632 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 10632 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 10632 58 3H-SPIPERONE -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 10632 58 UNDEFINED -33 30 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
25058166 222739 0 3H-YM 09151-2 -8 26 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-YM 09151-2 -8 26 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
1257 223157 0 3H-SPIPERONE 1 2 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCCC2C1CC3=C(C2)NN=C3 None
209 9831 97 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 9831 97 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 9831 97 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 9831 97 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 9831 97 3H-NEMONAPRIDE -30 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2448 106099 70 R-SAT -13 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 106099 70 R-SAT -13 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
None 223398 0 UNDEFINED -69 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 535 10 0 6 5.7 COC1=C(C=C(C=C1)C2=NOC(C2)CCCN3CCN(CC3)C(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F)OC None
1353 8692 93 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
4209 9937 75 None -562 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 None -562 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 None -562 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 None -562 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 None -562 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 None -562 33 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
1353 8692 93 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 8692 93 3H-SPIPERONE -4 85 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-SPIPERONE -4 85 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-SPIPERONE -4 85 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-SPIPERONE -4 85 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SPIPERONE -3 85 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-SPIPERONE -4 85 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
5280343 195054 124 None 1 31 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 195054 124 None 1 31 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 195054 124 None 1 31 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D4 receptorBinding affinity to dopamine D4 receptor
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
2812 11551 101 None -39 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 11551 101 None -39 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
2601 10552 33 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 10552 33 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 10552 33 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 10552 33 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 10552 33 3H-YM 09151-2 -7 21 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
176 7186 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 7186 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 7186 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 7186 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 7186 66 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
4189 213701 96 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 213701 96 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 213701 96 None -33 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
13091268 84999 0 UNDEFINED -8 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL210578 84999 0 UNDEFINED -8 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 401 6 1 3 5.0 O=C(CCCN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
2274 9947 58 UNDEFINED -56 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 UNDEFINED -56 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 UNDEFINED -56 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 UNDEFINED -56 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 UNDEFINED -56 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1016 10519 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 10519 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 10519 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 10519 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 10519 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 10519 78 None -28 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
54477 91428 36 None -14 22 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
Drug Central 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 91428 36 None -14 22 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-YM 09151 from human Dopamine receptor D4Displacement of [3H]-YM 09151 from human Dopamine receptor D4
Drug Central 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
3198 212292 76 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 212292 76 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 212292 76 None -26 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
1499 8872 47 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
3779 8872 47 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
536 8872 47 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
CHEMBL434 8872 47 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
DB01064 8872 47 None -18 17 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cellsDisplacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells
Drug Central 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C None
7077 73733 27 None -10 5 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL186720 73733 27 None -10 5 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL3925724 73733 27 None -10 5 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant dopamine receptor D4.4Binding affinity for human recombinant dopamine receptor D4.4
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
1830 9368 44 R-SAT -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 R-SAT -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 R-SAT -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 R-SAT -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 R-SAT -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 9368 44 None -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 9368 44 None -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 9368 44 None -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 9368 44 None -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 9368 44 None -120 28 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
2247 7293 81 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 7293 81 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 7293 81 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 7293 81 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 7293 81 None -63 42 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
1577 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
Binding affinity for Dopamine receptor D4Binding affinity for Dopamine receptor D4
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1577 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 10475 110 None -10 20 Human 8.3 pKi = 8.3 Binding
In vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cellsIn vitro displacement of [3H]spiperone from the recombinant human dopamine receptor D4 expressed in CHO cells
Drug Central 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2337 10030 77 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 None -114 62 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
103 10925 61 3H-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-SPIPERONE -4 53 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
219050 10146 25 3H-SPIPERONE -58 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 10146 25 3H-SPIPERONE -58 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 10146 25 3H-SPIPERONE -58 21 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
3117 214620 103 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 214620 103 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
1212 8443 50 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 8443 50 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-SPIPERONE -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 UNDEFINED -77 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
135398745 9688 112 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 UNDEFINED -10 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 223399 0 UNDEFINED -102 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 453 10 0 7 4.2 CCOC1=CC=CC=C1N2CCN(CC2)CCCC3CC(=NO3)C4=CC(=C(C=C4)OC)OC None
37459 7533 13 3H-SPIPERONE -123 24 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 7533 13 3H-SPIPERONE -123 24 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 7533 13 3H-SPIPERONE -123 24 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
242 7258 124 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-NMSP -87 51 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
44591088 196361 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL514591 196361 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.6 O=C(CCCN1CC2CC1N(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
242 7258 124 3H-NMSP -104 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-NMSP -104 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-NMSP -104 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-NMSP -104 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-NMSP -104 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
164512405 222728 0 3H-SPIPERONE -33 12 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
44578446 188359 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 None
CHEMBL476934 188359 0 UNDEFINED -3 3 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 372 6 0 3 4.4 O=C(CCCN1CC2CC1CN2c1ccc(Cl)cc1)c1ccc(F)cc1 None
9429 208912 58 3H-SPIPERONE -251 4 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 None
CHEMBL609109 208912 58 3H-SPIPERONE -251 4 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 None
135398737 7745 93 3H-N-Methylspiperone -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-N-Methylspiperone -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-N-Methylspiperone -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-N-Methylspiperone -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-N-Methylspiperone -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5311189 211620 11 3H-NMSP -1 27 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 211620 11 3H-NMSP -1 27 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
135398737 7745 93 UNDEFINED -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 UNDEFINED -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 UNDEFINED -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 UNDEFINED -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 UNDEFINED -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1577 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 10475 110 R-SAT -10 20 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
115237 62359 119 3H-NMSP -83 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-NMSP -83 54 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
135398737 7745 93 3H-SPIPERONE -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIPERONE -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIPERONE -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIPERONE -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIPERONE -13 90 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
185 10778 60 3H-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 10778 60 3H-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 10778 60 3H-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 10778 60 3H-SPIPERONE -7244 37 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
202478 211466 20 3H-YM 09151-2 -3 25 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 211466 20 3H-YM 09151-2 -3 25 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
1621 9207 17 3H-NMSP -181 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 3H-NMSP -181 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 3H-NMSP -181 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 3H-NMSP -181 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 3H-NMSP -181 44 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
22065962 183575 0 UNDEFINED 20 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 None
CHEMBL460644 183575 0 UNDEFINED 20 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 294 3 1 5 1.7 c1cnc(N2CCN(Cc3c[nH]c4ncccc34)CC2)nc1 None
None 223120 0 3H-SPIPERONE -74 19 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
10060538 11348 7 3H-SPIPERONE -3890 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
CHEMBL102582 11348 7 3H-SPIPERONE -3890 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
2105 9828 37 3H-SPIPERONE -11 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 3H-SPIPERONE -11 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 3H-SPIPERONE -11 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 3H-SPIPERONE -11 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 3H-SPIPERONE -11 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
44591087 182529 0 UNDEFINED -1 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 None
CHEMBL458342 182529 0 UNDEFINED -1 3 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 366 3 1 3 4.5 Clc1ccc(N2CCC3CCC(C2)N3Cc2c[nH]c3ncccc23)cc1 None
33630 185736 99 None -13 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 185736 99 None -13 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assayDisplacement of [3H]N-methylspiperone from human dopamine D4 receptor by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
2402 10143 62 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 10143 62 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 10143 62 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 10143 62 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 10143 62 None -1 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
681 8247 72 UNDEFINED -2 38 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 UNDEFINED -2 38 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 UNDEFINED -2 38 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 UNDEFINED -2 38 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 UNDEFINED -2 38 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
3191 109635 97 None -10 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 109635 97 None -10 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)DRUGMATRIX: Dopamine D4.2 radioligand binding (ligand: [3H] Spiperone)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
15387 52596 55 None -35 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 52596 55 None -35 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
31101 7516 40 None -186 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 None -186 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 None -186 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 None -186 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 None -186 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
212 10578 47 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 10578 47 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 10578 47 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 10578 47 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 10578 47 UNDEFINED -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
104870 105656 47 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 105656 47 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 105656 47 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
1153 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 8409 58 None -16 10 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
2202 9906 96 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 9906 96 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 9906 96 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 9906 96 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 9906 96 None -2 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
10065083 38877 1 UNDEFINED 1 10 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 None
CHEMBL140872 38877 1 UNDEFINED 1 10 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 328 6 0 5 2.4 O=C(CCCN1CCN(c2ncccn2)CC1)c1ccc(F)cc1 None
46 9680 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
71351 9680 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
CHEMBL2104619 9680 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
DB06229 9680 0 R-SAT -33 5 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C None
11653679 187970 1 UNDEFINED 3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476108 187970 1 UNDEFINED 3 11 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
242 7258 124 None -104 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 None -104 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 None -104 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 None -104 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 None -104 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
212 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
11154555 7587 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
5037 7587 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
7671 7587 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL2028019 7587 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL3085826 7587 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB06016 7587 62 None -501 12 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assayDisplacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
21302490 119582 32 None -12 9 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3233142 119582 32 None -12 9 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3306803 119582 32 None -12 9 Human 8.2 pKi = 8.2 Binding
Inhibition of human dopamine D4 receptorInhibition of human dopamine D4 receptor
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
135398745 9688 112 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-N-Methylspiperone -10 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
6852400 222716 0 3H-SPIPERONE -794 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 222716 0 3H-SPIPERONE -794 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
25139331 176707 0 UNDEFINED 1 4 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
CHEMBL444128 176707 0 UNDEFINED 1 4 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 None
3033769 10054 61 3H-RACLOPRIDE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 10054 61 3H-SPIPERONE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 10054 61 UNDEFINED -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 3H-RACLOPRIDE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 3H-SPIPERONE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 10054 61 UNDEFINED -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 3H-RACLOPRIDE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 3H-SPIPERONE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 10054 61 UNDEFINED -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 3H-RACLOPRIDE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 3H-SPIPERONE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 10054 61 UNDEFINED -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 3H-RACLOPRIDE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 3H-SPIPERONE -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 10054 61 UNDEFINED -562 18 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
44134711 222770 0 3H-Methylspiperone -724 13 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
None 222909 0 3H-YM 09151-2 -8 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 273 6 0 2 4.3 CCCN(CCC)C1C=CC2=C(C1C)C=CC=C2OC None
25139481 191619 0 UNDEFINED -4 4 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 None
CHEMBL485227 191619 0 UNDEFINED -4 4 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 None
25139477 191024 0 UNDEFINED -15 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 None
CHEMBL483593 191024 0 UNDEFINED -15 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 None
44123782 196379 0 UNDEFINED -6 3 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 None
CHEMBL514747 196379 0 UNDEFINED -6 3 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 1 3 3.7 Clc1ccc(N2CC3CC2CN3Cc2c[nH]c3ncccc23)cc1 None
2477 7532 59 None -1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 7532 59 None -1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 7532 59 None -1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 7532 59 None -1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 7532 59 None -1 29 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2389 10104 118 3H-SPIPERONE -22 66 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 10104 118 3H-SPIROPERIDOL -22 66 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SPIPERONE -22 66 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SPIROPERIDOL -22 66 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SPIPERONE -22 66 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SPIROPERIDOL -22 66 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SPIPERONE -22 66 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SPIROPERIDOL -22 66 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SPIPERONE -22 66 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SPIROPERIDOL -22 66 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1212 8443 50 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 R-SAT -77 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2274 9947 58 None -56 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 None -56 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 None -56 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 None -56 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 None -56 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1621 9207 17 None -64 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 None -64 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 None -64 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 None -64 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 None -64 44 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D4Binding affinity towards Dopamine receptor D4
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2105 9828 37 None -11 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 None -11 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 None -11 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 None -11 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 None -11 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2407 10145 76 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
59227 10145 76 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
941 10145 76 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
CHEMBL1303 10145 76 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
DB05271 10145 76 None -30 7 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.Binding affinity was evaluated by calculating competition for [3H]spiperone binding on Dopamine receptor D4.2 of CHO K-1 cells.
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
115237 62359 119 None -83 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 None -83 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
242 7258 124 None -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 None -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 None -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 None -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 None -87 51 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
37 7565 60 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 7565 60 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 7565 60 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 7565 60 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 7565 60 None -7 17 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
135398745 9688 112 None -7 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 None -7 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 None -7 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 None -7 65 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2865 10915 73 None -66 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 None -66 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 None -66 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 None -66 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 None -66 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
49831411 224525 0 None -1 15 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 659 19 0 6 8.7 CCCCCCCCCCCC(=O)OCN1C(=O)CCC2=CC=C(OCCCCN3CCN(CC3)C3=C(Cl)C(Cl)=CC=C3)C=C12 None
49831411 224525 0 None -1 15 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 659 19 0 6 8.7 CCCCCCCCCCCC(=O)OCN1C(=O)CCC2=CC=C(OCCCCN3CCN(CC3)C3=C(Cl)C(Cl)=CC=C3)C=C12 None
214 10632 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 10632 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 10632 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 10632 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 10632 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 10632 58 None -33 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
103 10925 61 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 None -17 53 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine-4.2 receptorBinding affinity towards human dopamine-4.2 receptor
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
3389 224490 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
191 7191 98 None -8 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 7191 98 None -8 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 7191 98 None -8 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 7191 98 None -8 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 7191 98 None -8 29 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation countingDisplacement of [3H]-YM09151-2 from human cloned dopamine D4 receptor expressed in insect Sf9 cells after 60 mins by liquid scintillation counting
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2389 10104 118 3H-SPIPERONE -30 66 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SPIPERONE -30 66 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SPIPERONE -30 66 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SPIPERONE -30 66 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SPIPERONE -30 66 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
135398737 7745 93 None -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
16106 124924 34 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 124924 34 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
1212 8443 50 None -77 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 None -77 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 None -77 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 None -77 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 None -77 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
209 9831 97 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 9831 97 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 9831 97 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 9831 97 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 9831 97 None -30 23 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
3294 8787 111 None -11 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 None -11 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 None -11 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 None -11 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 None -11 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
135398737 7745 93 R-SAT -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 R-SAT -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 R-SAT -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 R-SAT -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 R-SAT -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
65750 223225 0 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 346 6 0 3 5.7 CCN(CC)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl None
2726 7706 68 None -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 None -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 None -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 None -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 None -8 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1443 8809 34 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
33625 8809 34 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
501 8809 34 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
CHEMBL279516 8809 34 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
DB08950 8809 34 None -1 11 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 347 5 2 2 3.6 O=C(c1ccccc1)NC1CCN(CC1)CCc1c[nH]c2c1cccc2 None
2448 106099 70 None -13 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
CHEMBL28218 106099 70 None -13 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 None
1613 9127 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1613 9127 53 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 UNDEFINED -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
5280343 195054 124 UNDEFINED 1 31 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 195054 124 UNDEFINED 1 31 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 195054 124 UNDEFINED 1 31 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
5467 212707 43 None 6 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
CHEMBL84158 212707 43 None 6 5 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 328 8 1 5 1.2 CCN(CC)CCNC(=O)c1cc(S(C)(=O)=O)ccc1OC None
16106 124924 34 3H-SPIPERONE 1 11 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
CHEMBL340801 124924 34 3H-SPIPERONE 1 11 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 291 0 0 3 2.9 CN1CCN(C2=Nc3ccccc3Cc3ccccc32)CC1 None
2435 10362 83 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 None -10 48 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cellsDisplacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
100 10577 58 None -8 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 None -8 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 None -8 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 None -8 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 None -8 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
135409468 8816 69 R-SAT -18 39 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 8816 69 R-SAT -18 39 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 8816 69 R-SAT -18 39 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
2274 9947 58 3H-SPIPERONE -56 31 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 3H-SPIPERONE -56 31 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 3H-SPIPERONE -56 31 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 3H-SPIPERONE -56 31 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 3H-SPIPERONE -56 31 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
15387 52596 55 3H-SPIPERONE -35 24 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 52596 55 3H-SPIPERONE -35 24 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
213 10625 55 3H-NMSP -6 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 10625 55 3H-NMSP -6 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 10625 55 3H-NMSP -6 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 10625 55 3H-NMSP -6 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 10625 55 3H-NMSP -6 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
6450478 222791 0 3H-SPIPERONE -18 12 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 340 0 0 6 3.4 CN1CCN(CC1)C2=NC3=CSC=C3C(=CC#N)C4=CSC=C42 None
11954259 222758 0 3H-SPIPERONE -257 43 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
5280343 195054 124 3H-Methylspiperone -114 31 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 195054 124 3H-Methylspiperone -114 31 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 195054 124 3H-Methylspiperone -114 31 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
44591086 196360 0 UNDEFINED -61 3 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 None
CHEMBL514590 196360 0 UNDEFINED -61 3 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 367 3 2 3 4.2 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2Cc1c[nH]c2ncccc12 None
44395709 181677 0 UNDEFINED 1 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL456429 181677 0 UNDEFINED 1 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
CHEMBL556361 181677 0 UNDEFINED 1 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 4 1 3 4.2 O=C(CN1C2CCC1CC(O)(c1ccc(Cl)cc1)C2)c1ccc(F)cc1 None
2389 10104 118 None -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 None -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 None -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 None -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 None -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1712 9270 43 None -2 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 9270 43 None -2 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 9270 43 None -2 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 9270 43 None -2 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 9270 43 None -2 22 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
135398737 7745 93 None -7 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -7 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -7 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -7 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -7 90 Rat 8.1 pKi = 8.1 Binding
Binding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brainBinding affinity of [3H]-spiperone towards cloned mammalian Dopamine receptor D4 expressed in cultured cells or from rat whole brain
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
228 7233 28 None -1 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 7233 28 None -1 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 7233 28 None -1 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 7233 28 None -1 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 7233 28 None -1 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membraneDisplacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
1222 8445 49 None -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 None -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 None -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 None -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 None -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2601 10552 33 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 10552 33 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 10552 33 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 10552 33 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 10552 33 None -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
4249 84954 34 None -7 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 84954 34 None -7 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
2601 10552 33 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 10552 33 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 10552 33 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 10552 33 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 10552 33 3H-SPIPERONE -7 21 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
2563 10523 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
55 10523 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
91273 10523 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
CHEMBL274047 10523 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
DB12833 10523 59 None 1 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to Dopamine receptor D4 was determinedBinding affinity to Dopamine receptor D4 was determined
Drug Central 383 6 0 6 1.4 O=C1N(CCCCN2CCN(CC2)c2ncccn2)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 None
11978813 7508 79 None -10 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 7508 79 None -10 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 7508 79 None -10 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 7508 79 None -10 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 7508 79 None -10 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
52919 21222 48 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1200986 21222 48 None -3 4 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
1588 9105 27 None -16 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 None -16 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 None -16 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 None -16 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 None -16 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
1613 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
Affinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptorAffinity was evaluated by inhibition of [3H]-spiperone binding to COS cells transfected with human dopamine D-4 receptor
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
5022 8432 76 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
6918248 8432 76 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
8182 8432 76 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
CHEMBL231068 8432 76 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
DB04908 8432 76 None -1 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
1524 8962 96 None -4 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 None -4 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 None -4 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 None -4 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 None -4 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 None -4 51 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human dopamine receptor D4Binding affinity towards human dopamine receptor D4
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2780 117306 36 None -4 10 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
CHEMBL325109 117306 36 None -4 10 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cellsAbility to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
2389 10104 118 UNDEFINED -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 UNDEFINED -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 UNDEFINED -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 UNDEFINED -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 UNDEFINED -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
25058166 222739 0 3H-SPIPERONE -8 26 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-SPIPERONE -8 26 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
2389 10104 118 3H-N-Methylspiperone -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-N-Methylspiperone -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-N-Methylspiperone -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-N-Methylspiperone -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-N-Methylspiperone -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
16363 7383 53 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
312 7383 53 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
9215 7383 53 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL297302 7383 53 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB12867 7383 53 None -1 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
46780481 114308 20 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 None -23 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
16362 9899 71 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 9899 71 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 9899 71 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 9899 71 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 9899 71 None -20 29 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
135398745 9688 112 None -10 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 None -10 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 None -10 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 None -10 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1222 8445 49 R-SAT -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 R-SAT -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 R-SAT -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 R-SAT -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 R-SAT -14 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
15387 52596 55 3H-NEMONAPRIDE -35 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1531134 52596 55 3H-NEMONAPRIDE -35 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
44591043 183591 0 UNDEFINED 3 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 None
CHEMBL460855 183591 0 UNDEFINED 3 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 3 2 2 3.9 OC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)C1 None
None 222793 0 3H-SPIPERONE -85 3 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 411 6 1 3 3.9 C1CCC(CC1)NC(=O)N2CCN(CC2)CCCC(=O)C3=CC=C(C=C3)F.Cl None
2402 10143 62 3H-SPIPERONE -1 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 10143 62 3H-SPIPERONE -1 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 10143 62 3H-SPIPERONE -1 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 10143 62 3H-SPIPERONE -1 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 10143 62 3H-SPIPERONE -1 24 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
10060538 11348 7 3H-SPIPERONE -3890 4 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
CHEMBL102582 11348 7 3H-SPIPERONE -3890 4 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 247 2 1 3 2.5 CCCN1CCOC2c3cc(O)ccc3CCC21 None
None 223210 0 3H-SPIPERONE -165 3 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 160 1 0 2 2.6 CC(=O)C1=CC2=CC=CC=C2O1 None
681 8247 72 None -2 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 None -2 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 None -2 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 None -2 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 None -2 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
135398737 7745 93 3H-SPIPERONE -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIPERONE -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIPERONE -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIPERONE -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIPERONE -13 90 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 9127 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-SPIPERONE -2 44 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
2389 10104 118 3H-SCH23390 -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-SCH23390 -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-SCH23390 -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-SCH23390 -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-SCH23390 -22 66 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2435 10362 83 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-SPIPERONE -10 48 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
3168 16034 92 None -4 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 16034 92 None -4 22 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
1712 9270 43 R-SAT -2 22 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 9270 43 R-SAT -2 22 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 9270 43 R-SAT -2 22 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 9270 43 R-SAT -2 22 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 9270 43 R-SAT -2 22 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
1212 8443 50 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-SPIPERONE -18 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
119570 9933 96 None -6 39 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 None -6 39 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 None -6 39 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 None -6 39 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 None -6 39 Human 8.0 pKi = 8.0 Binding
in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand.
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
1238 209953 24 None -2 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 209953 24 None -2 16 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
2726 7706 68 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SPIPERONE -8 72 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
135398737 7745 93 3H-SPIPERONE -7 90 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-SPIPERONE -7 90 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-SPIPERONE -7 90 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-SPIPERONE -7 90 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-SPIPERONE -7 90 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398745 9688 112 3H-SPIPERONE -7 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-SPIPERONE -7 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-SPIPERONE -7 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-SPIPERONE -7 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2470 10425 50 None -20 58 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 None -20 58 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 None -20 58 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 None -20 58 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 None -20 58 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [3H]Spiperone from human recombinant dopamine D4 receptor expressed in CHOK1 cells after 2 hrs
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2726 7706 68 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-SPIPERONE -10 72 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
191 7191 98 3H-SPIPERONE -67 29 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 7191 98 3H-SPIPERONE -67 29 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 7191 98 3H-SPIPERONE -67 29 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 7191 98 3H-SPIPERONE -67 29 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 7191 98 3H-SPIPERONE -67 29 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
None 223210 0 3H-SPIPERONE -165 3 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 160 1 0 2 2.6 CC(=O)C1=CC2=CC=CC=C2O1 None
164512405 222728 0 3H-SPIPERONE -10 12 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)C2=C(C=CC(=C2)S(=O)(=O)N)OC None
202478 211466 20 3H-NMSP -3 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 211466 20 3H-NMSP -3 25 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
115368 9830 47 None 1 4 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
2112 9830 47 None 1 4 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
7556 9830 47 None 1 4 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
CHEMBL1472975 9830 47 None 1 4 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
DB08922 9830 47 None 1 4 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 9577836
16363 7383 53 None -1 7 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
312 7383 53 None -1 7 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
9215 7383 53 None -1 7 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
CHEMBL297302 7383 53 None -1 7 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
DB12867 7383 53 None -1 7 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 9577836
1577 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
2537 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5355 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5501 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
643497 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
688272 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
958 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
960 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL196677 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL26 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL267044 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB00391 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB16021 10475 110 None -10 20 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
3033769 10054 61 None -288 18 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
3299 10054 61 None -288 18 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
94 10054 61 None -288 18 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
CHEMBL8809 10054 61 None -288 18 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
DB12518 10054 61 None -288 18 Rat 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10617689
16094676 7020 19 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 17149874
8439 7020 19 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 17149874
CHEMBL219182 7020 19 None - 1 Human 5.8 pKi = 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 325 4 1 3 2.2 Cc1cccc(c1)C(=O)NCN1CCC(CC1)c1cccc[n+]1[O-] 17149874
2274 9947 58 None -56 31 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 None -56 31 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 None -56 31 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 None -56 31 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 None -56 31 Human 6.1 pKi = 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
31101 7516 40 None -186 35 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
35 7516 40 None -186 35 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
403 7516 40 None -186 35 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
CHEMBL493 7516 40 None -186 35 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
DB01200 7516 40 None -186 35 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
1577 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
1577 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
2537 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
2537 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5355 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
5355 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
5501 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
5501 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
643497 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
643497 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
688272 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
688272 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
958 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
958 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
960 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
960 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL196677 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
CHEMBL196677 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL26 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
CHEMBL26 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
CHEMBL267044 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
CHEMBL267044 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB00391 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
DB00391 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
DB16021 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8301592
DB16021 10475 110 None -10 20 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 341 6 2 5 0.6 CCN1CCC[C@@H]1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 8967990
2407 10145 76 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
59227 10145 76 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
941 10145 76 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
CHEMBL1303 10145 76 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
DB05271 10145 76 None -30 7 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 8863800
214 10632 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
2740 10632 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
5566 10632 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
66064 10632 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
CHEMBL422 10632 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
DB00831 10632 58 None -33 30 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 9015795
103 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
2875 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
5736 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
CHEMBL285802 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
DB09225 10925 61 None -17 53 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
72737723 9356 1 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 25221667
8440 9356 1 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 25221667
CHEMBL3335556 9356 1 None - 1 Human 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 5 0 2 4.2 Clc1ccc(cc1)CN1CCO[C@@H](C1)CCc1ccccc1 25221667
2 10035 23 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
2 10035 23 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 1840645
2 10035 23 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 8967990
54562 10035 23 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
54562 10035 23 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 1840645
54562 10035 23 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 8967990
CHEMBL240773 10035 23 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 12388666
CHEMBL240773 10035 23 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 1840645
CHEMBL240773 10035 23 None -2 28 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 8967990
681 8247 72 None -2 38 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
940 8247 72 None -2 38 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
947 8247 72 None -2 38 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
CHEMBL59 8247 72 None -2 38 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
DB00988 8247 72 None -2 38 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1840645
3251 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
5684 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
80 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
CHEMBL31354 10844 58 None -43 12 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 21520940
10425450 6989 30 None -1 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
10425450 6989 30 None 1 4 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
3301 6989 30 None -1 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
3301 6989 30 None 1 4 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
CHEMBL375596 6989 30 None -1 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
CHEMBL375596 6989 30 None 1 4 Rat 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 309 4 1 3 3.2 O=C(Nc1cccc(c1)C)CN1CCC(CC1)c1ccccn1 16153699
1613 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
205 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
3964 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
CHEMBL831 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
DB00408 9127 53 None -2 44 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 9015795
228 7233 28 None -1 23 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
33 7233 28 None -1 23 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
6005 7233 28 None -1 23 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
CHEMBL53 7233 28 None -1 23 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
DB00714 7233 28 None -1 23 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 12388666
2435 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
2435 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
2435 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
60149 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
60149 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
60149 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
98 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
98 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
98 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
CHEMBL12713 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
CHEMBL12713 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
CHEMBL12713 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
DB06144 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 16135699
DB06144 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9015795
DB06144 10362 83 None -10 48 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 9577836
133008 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 8642551
3302 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 8642551
CHEMBL444309 9022 22 None 204 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 5 0 3 5.7 Clc1ccc(cc1)c1onc(c1C)C1CCN(CC1)CCc1ccccc1 8642551
1353 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
1353 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
1353 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
3559 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
3559 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
3559 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
86 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
86 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
86 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
CHEMBL54 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
CHEMBL54 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
CHEMBL54 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
DB00502 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
DB00502 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 7862709
DB00502 8692 93 None -3 85 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 8102973
3645619 9808 20 None 5 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 15448188
975 9808 20 None 5 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 15448188
CHEMBL45244 9808 20 None 5 9 Rat 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 15448188
11301655 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 15992586
8441 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 15992586
CHEMBL127257 6988 37 None 245 4 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 3 1 3 3.5 Cc1ccc(cc1C)N1CCN(CC1)Cc1nc2c([nH]1)cccc2 15992586
133079 10410 42 None 1 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 9098699
980 10410 42 None 1 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 9098699
CHEMBL69759 10410 42 None 1 3 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 9098699
5615 10671 8 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 9098699
5781 10671 8 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 9098699
CHEMBL1179189 10671 8 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 339 6 0 4 4.0 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccccc1)C)C 9098699
3303 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 8642550
5311200 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 8642550
CHEMBL267014 9024 46 None 1 15 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 8642550
179 7188 115 None -50 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 None -50 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 None -50 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 None -50 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 None -50 50 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
243 9976 91 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 9976 91 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 9976 91 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 9976 91 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 9976 91 None -12 34 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
213 10625 55 None -6 43 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 10625 55 None -6 43 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 10625 55 None -6 43 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 10625 55 None -6 43 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 10625 55 None -6 43 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2342 7386 39 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
331 7386 39 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
7124 7386 39 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
CHEMBL1201250 7386 39 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
DB00767 7386 39 None -1 6 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 404 6 0 6 2.4 CCN(C(=O)C1CN2CCc3c(C2CC1OC(=O)C)cc(c(c3)OC)OC)CC None
5281878 8441 35 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 8441 35 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 8441 35 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 8441 35 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 8441 35 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 8441 35 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 8441 35 None -14 16 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
11976 7707 59 None -2 24 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 7707 59 None -2 24 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 7707 59 None -2 24 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 7707 59 None -2 24 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
5567 49576 27 None -11 8 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 49576 27 None -11 8 Human 8.0 pKi None 8.0 Binding
NoneNone
Drug Central 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
6603897 9027 22 None 5 2 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10617689
978 9027 22 None 5 2 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10617689
CHEMBL60518 9027 22 None 5 2 Rat 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 418 3 1 3 3.5 Ic1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10617689
37459 7533 13 None -123 24 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 8967990
62 7533 13 None -123 24 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 8967990
CHEMBL8514 7533 13 None -123 24 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 8967990
3408722 9491 45 None -1318 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 7 1 4 3.7 CCCCN1CCCC1CNC(=O)c1cc(C#N)c2c(c1OC)cccc2 10617689
44 9491 45 None -1318 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 7 1 4 3.7 CCCCN1CCCC1CNC(=O)c1cc(C#N)c2c(c1OC)cccc2 10617689
CHEMBL286252 9491 45 None -1318 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 7 1 4 3.7 CCCCN1CCCC1CNC(=O)c1cc(C#N)c2c(c1OC)cccc2 10617689
1153 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
12668023 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
30026874 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
30026875 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
3341 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
6603851 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
933 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
939 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
985 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
CHEMBL1160786 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
CHEMBL1161520 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
CHEMBL588 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
DB00800 8409 58 None -16 10 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1840645
2202 9906 96 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
4850 9906 96 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
49 9906 96 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
CHEMBL1371770 9906 96 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
DB12478 9906 96 None -2 21 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 12388666
57267 8374 14 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
966 8374 14 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
CHEMBL8946 8374 14 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
DB15492 8374 14 None -416 4 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 6 2 4 2.8 CCN1CCC[C@H]1CNC(=O)c1c(O)c(CC)cc(c1OC)Cl 7475902
2105 9828 37 None -11 32 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 9828 37 None -11 32 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 9828 37 None -11 32 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 9828 37 None -11 32 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 9828 37 None -11 32 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
242 7258 124 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
34 7258 124 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
60795 7258 124 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
CHEMBL1112 7258 124 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
DB01238 7258 124 None -87 51 Rat 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10617689
37 7565 60 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 7565 60 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 7565 60 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 7565 60 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 7565 60 None -7 17 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
681 8247 72 None -7 38 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
940 8247 72 None -7 38 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
947 8247 72 None -7 38 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
CHEMBL59 8247 72 None -7 38 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
DB00988 8247 72 None -7 38 Rat 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10617689
135398737 7745 93 None -13 90 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
38 7745 93 None -13 90 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
722 7745 93 None -13 90 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
CHEMBL42 7745 93 None -13 90 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
DB00363 7745 93 None -13 90 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8102973
2726 7706 68 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
621 7706 68 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
83 7706 68 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
CHEMBL71 7706 68 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
DB00477 7706 68 None -8 72 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 8102973
11429930 10114 0 None - 1 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 415 8 3 7 1.9 COc1cc(ccc1O)N1CCN(CC1)CC(COc1ccccc1NC(=O)C)O 15448188
982 10114 0 None - 1 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 415 8 3 7 1.9 COc1cc(ccc1O)N1CCN(CC1)CC(COc1ccccc1NC(=O)C)O 15448188
2601 10552 33 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
443951 10552 33 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
56 10552 33 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL73151 10552 33 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB13399 10552 33 None -7 21 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
219050 10146 25 None -58 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
52 10146 25 None -58 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
CHEMBL431367 10146 25 None -58 21 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
1588 9105 27 None -16 44 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 9105 27 None -16 44 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 9105 27 None -16 44 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 9105 27 None -16 44 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 9105 27 None -16 44 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
133079 10410 42 None -1 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 15448188
980 10410 42 None -1 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 15448188
CHEMBL69759 10410 42 None -1 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 5 1 5 2.2 NS(=O)(=O)c1ccc(cc1)N1CCN(CC1)CC[C@@H]1OCCc2c1cccc2 15448188
10336538 8406 50 None 3 8 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 15448188
974 8406 50 None 3 8 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 15448188
CHEMBL310843 8406 50 None 3 8 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 15448188
2470 10425 50 None -20 58 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
3300 10425 50 None -20 58 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
5265 10425 50 None -20 58 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
99 10425 50 None -20 58 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
CHEMBL267930 10425 50 None -20 58 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 7475902
973 7960 39 None 9 6 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 15448188
9796720 7960 39 None 9 6 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 15448188
CHEMBL77395 7960 39 None 9 6 Rat 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 310 3 1 3 3.0 Fc1ccc2c(c1)cc([nH]2)CN1CCN(CC1)c1ccccn1 15448188
977 7961 5 None 10 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 15448188
9820261 7961 5 None 10 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 15448188
CHEMBL66227 7961 5 None 10 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 4 0 5 2.7 Fc1ccc(cc1)OC[C@@H]1CC[C@@H]2N(C1)CCN(C2)c1ncc(cn1)F 15448188
188942 9594 41 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
3297 9594 41 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
979 9594 41 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
CHEMBL103772 9594 41 None 12 4 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 320 4 1 5 2.2 c1ccc(cc1)c1ncc([nH]1)CN1CCN(CC1)c1ncccn1 15448188
5041 10067 6 None 1 6 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 15448188
981 10067 6 None 1 6 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 15448188
CHEMBL4096543 10067 6 None 1 6 Rat 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 15448188