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
Sel. page Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

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

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL5077128 221262 7 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assayAgonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assay
ChEMBL None None None CS(=O)(=O)C1(CNCc2cccc3cccnc23)CC1 10.1021/acs.jmedchem.1c02031
CHEMBL5082447 221582 2 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assayAgonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assay
ChEMBL None None None CS(=O)(=O)C1(CNCc2ccc(Cl)c3cccnc23)CC1 10.1021/acs.jmedchem.1c02031
785909 47822 7 None 1 2 Human 4.3 pEC50 = 4.3 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 336 4 1 3 4.1 COc1ccc(CN2CCc3c([nH]c4ccccc34)C2)c(OC)c1C nan
CHEMBL1487650 47822 7 None 1 2 Human 4.3 pEC50 = 4.3 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 336 4 1 3 4.1 COc1ccc(CN2CCc3c([nH]c4ccccc34)C2)c(OC)c1C nan
1765347 62893 13 None -1 2 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C nan
CHEMBL1606743 62893 13 None -1 2 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C nan
CHEMBL1625496 62893 13 None -1 2 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 324 7 2 3 3.8 COc1ccc(CNCCc2c[nH]c3ccccc23)c(OC)c1C nan
253793 17328 45 None -1 2 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 594 2 2 8 6.6 COc1cc2c3cc1Oc1cc(ccc1O)C[C@@H]1c4c(cc(OC)c(O)c4Oc4ccc(cc4)C[C@H]3N(C)CC2)CCN1C nan
CHEMBL1169627 17328 45 None -1 2 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 594 2 2 8 6.6 COc1cc2c3cc1Oc1cc(ccc1O)C[C@@H]1c4c(cc(OC)c(O)c4Oc4ccc(cc4)C[C@H]3N(C)CC2)CCN1C nan
1795 8372 64 None -10 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
4186 8372 64 None -10 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
CHEMBL517986 8372 64 None -10 4 Human 4.1 pEC50 = 4.1 Functional
PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]PUBCHEM_BIOASSAY: Counterscreen for agonists of OPRM1-OPRD1 heterodimerization: luminescence-based cell-based high throughput dose response assay to identify agonists of 5-hydroxytryptamine (serotonin) 5A receptor (HTR5A). (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504326, AID504355, AID504692, AID504904, AID504905]
ChEMBL 299 4 3 5 0.4 CCN(c1nc(N)c(nc1Cl)C(=O)N=C(N)N)C(C)C nan
16006492 104245 7 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270177 104245 7 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
16006492 104245 7 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL270177 104245 7 None - 0 Human 8.5 pKd = 8.5 Functional
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
135458393 162375 4 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404511 162375 4 None - 0 Human 7.4 pKd = 7.4 Functional
Antagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assayAntagonist activity at human 5HT5A receptor by [35S]GTP-gamma-S binding assay
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
135458392 104201 5 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL269964 104201 5 None - 0 Human 8.1 pKd = 8.1 Functional
Antagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assayAntagonist activity at human recombinant 5HT5A receptor expressed in HEK293-EBNA cells by [35S]GTP-gamma-S binding assay
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
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

 LogP

 Smiles

 DOI
5329102 201505 86 None - 0 Human 5.0 pAC50 = 5 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 5.0 pAC50 = 5 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -77 85 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -77 85 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -77 85 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -77 85 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -77 85 Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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
1613 9127 53 None -19 44 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -19 44 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -19 44 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -19 44 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -19 44 Human 6.0 pAC50 = 6.0 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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
3158 63041 27 None - 20 Human 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 5.9 pAC50 = 5.9 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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
2247 7293 81 None - 42 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 - 42 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 - 42 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 - 42 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 - 42 Human 5.8 pAC50 = 5.8 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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
135409453 10545 41 None - 2 Human 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.7 pAC50 = 6.7 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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
1427 8794 54 None - 27 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -109 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -109 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -109 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 -109 65 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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
1400 8738 70 None - 3 Human 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.6 pAC50 = 6.6 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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
2726 7706 68 None -16 72 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 7706 68 None -16 72 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 7706 68 None -16 72 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 7706 68 None -16 72 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 7706 68 None -16 72 Human 6.4 pAC50 = 6.4 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
43815 193699 64 None - 25 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL1708 193699 64 None - 25 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
CHEMBL490 193699 64 None - 25 Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 10.1038/s41467-023-40064-9
21722 24764 31 None - 6 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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
191 7191 98 None - 29 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 - 29 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 - 29 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 - 29 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 - 29 Human 6.2 pAC50 = 6.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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
1224 8214 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
3100 8214 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
8980 8214 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
916 8214 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
CHEMBL657 8214 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
DB01075 8214 83 None - 13 Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtration
ChEMBL 255 6 0 2 3.4 CN(CCOC(c1ccccc1)c1ccccc1)C 10.1038/s41467-023-40064-9
2284 9956 33 None - 29 Human 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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 6.1 pAC50 = 6.1 Binding
Binding affinity towards human HTR5A in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HTR5A 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
44469677 21945 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cells
ChEMBL 336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2010.06.050
CHEMBL1210154 21945 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in CHO cells
ChEMBL 336 4 1 4 5.4 C/C(=N\OC(=O)Nc1ccccc1)c1cccc(-c2cccs2)c1 10.1016/j.bmcl.2010.06.050
10383252 11359 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3C(C)(C)CNS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL102645 11359 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3C(C)(C)CNS3(=O)=O)cc12 10.1021/jm00045a006
72548703 168346 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5a receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 168346 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5a receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
10404770 11488 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 336 6 2 3 1.0 CN(C)CCc1c[nH]c2ccc(CCN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL103549 11488 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 336 6 2 3 1.0 CN(C)CCc1c[nH]c2ccc(CCN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
10021702 116169 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 364 7 1 3 1.7 CCN1CCN(CCc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL321963 116169 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 364 7 1 3 1.7 CCN1CCN(CCc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
10043491 116601 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 1 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CCCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL323334 116601 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 1 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CCCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
5 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5202 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
CHEMBL39 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
DB08839 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cellsDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in HEK293 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
5202 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
CHEMBL39 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
DB08839 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
5 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 6927 72 None -323 53 Human 6.8 pIC50 = 6.8 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5 6927 72 None -323 53 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
5202 6927 72 None -323 53 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
CHEMBL39 6927 72 None -323 53 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
DB08839 6927 72 None -323 53 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human 5HT5A receptorInhibition of human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
10315894 11459 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 6 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CCN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL103371 11459 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 6 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CCN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
10412397 11460 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 469 8 2 4 2.8 CC(=O)Nc1ccc(CN2CCN(Cc3ccc4[nH]cc(CCN(C)C)c4c3)S2(=O)=O)cc1 10.1021/jm00045a006
CHEMBL103388 11460 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 469 8 2 4 2.8 CC(=O)Nc1ccc(CN2CCN(Cc3ccc4[nH]cc(CCN(C)C)c4c3)S2(=O)=O)cc1 10.1021/jm00045a006
10404070 85223 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 325 4 1 4 1.4 CN1CCN(Cc2ccc3scc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL2111620 85223 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 325 4 1 4 1.4 CN1CCN(Cc2ccc3scc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
10337965 115368 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CC(C)(C)NS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL320412 115368 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 350 5 2 3 1.7 CN(C)CCc1c[nH]c2ccc(CN3CC(C)(C)NS3(=O)=O)cc12 10.1021/jm00045a006
5 6927 72 None -323 53 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 6927 72 None -323 53 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 6927 72 None -323 53 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 6927 72 None -323 53 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5 6927 72 None -323 53 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
5202 6927 72 None -323 53 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
CHEMBL39 6927 72 None -323 53 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
DB08839 6927 72 None -323 53 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human 5-HT5A receptor by radioligand displacement assayBinding affinity to human 5-HT5A receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
10885636 117793 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
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 5.5 pIC50 = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
2543 10479 68 None -1412 32 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
5358 10479 68 None -1412 32 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
54 10479 68 None -1412 32 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
CHEMBL128 10479 68 None -1412 32 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
DB00669 10479 68 None -1412 32 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00045a006
9998879 114277 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 364 6 1 3 2.0 CC(C)N1CCN(Cc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL318571 114277 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 364 6 1 3 2.0 CC(C)N1CCN(Cc2ccc3[nH]cc(CCN(C)C)c3c2)S1(=O)=O 10.1021/jm00045a006
11730467 17800 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
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 5.3 pIC50 = 5.3 Binding
Binding affinity against 5-hydroxytryptamine 5A receptorBinding affinity against 5-hydroxytryptamine 5A receptor
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
11722814 11534 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 308 4 2 3 0.7 CN1CCN(Cc2ccc3[nH]cc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
CHEMBL103854 11534 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 308 4 2 3 0.7 CN1CCN(Cc2ccc3[nH]cc(CCN)c3c2)S1(=O)=O 10.1021/jm00045a006
10245588 114604 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 4 1 3 1.3 CN(C)CCc1c[nH]c2ccc(N3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL319223 114604 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 4 1 3 1.3 CN(C)CCc1c[nH]c2ccc(N3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
5 6927 72 None -323 53 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
5202 6927 72 None -323 53 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
CHEMBL39 6927 72 None -323 53 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
DB08839 6927 72 None -323 53 Human 7.1 pIC50 = 7.1 Binding
Percent inhibition against 5-hydroxytryptamine 5A receptor at 1 uMPercent inhibition against 5-hydroxytryptamine 5A receptor at 1 uM
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm058018d
10340828 11136 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 398 6 1 3 2.8 CN(C)CCc1c[nH]c2ccc(N3CCN(Cc4ccccc4)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL101138 11136 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 398 6 1 3 2.8 CN(C)CCc1c[nH]c2ccc(N3CCN(Cc4ccccc4)S3(=O)=O)cc12 10.1021/jm00045a006
10471382 11344 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 5 2 3 0.9 CN(C)CCc1c[nH]c2ccc(CN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL102548 11344 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 5 2 3 0.9 CN(C)CCc1c[nH]c2ccc(CN3CCNS3(=O)=O)cc12 10.1021/jm00045a006
10471383 11350 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 5 2 3 0.9 CNCCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL102586 11350 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 322 5 2 3 0.9 CNCCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
9819150 11440 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 336 5 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
CHEMBL103205 11440 2 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
ChEMBL 336 5 1 3 1.3 CN(C)CCc1c[nH]c2ccc(CN3CCN(C)S3(=O)=O)cc12 10.1021/jm00045a006
60152964 133568 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
CHEMBL3654198 133568 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
60151043 133576 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3c(F)cccc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654206 133576 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3c(F)cccc3F)ccc(F)c2C2(CC2)C1 nan
3233 10285 44 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
3247 10285 44 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
6604889 10285 44 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
CHEMBL282199 10285 44 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
DB13988 10285 44 None -10 12 Human 9.1 pKi = 9.1 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/acs.jmedchem.1c01093
60151044 133582 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654212 133582 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 374 1 2 1 3.0 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
60151042 133578 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3c(F)cc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654208 133578 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3c(F)cc(F)cc3F)ccc(F)c2C2(CC2)C1 nan
91819725 133584 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 356 1 2 1 2.9 NC(N)=NC(=O)N1Cc2c(-c3ccccc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654214 133584 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 356 1 2 1 2.9 NC(N)=NC(=O)N1Cc2c(-c3ccccc3F)ccc(F)c2C2(CC2)C1 nan
4106 9280 22 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 9280 22 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 9280 22 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 9280 22 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
4106 9280 22 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 9280 22 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 9280 22 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 9280 22 None -14 33 Human 9.0 pKi = 9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
60150902 133567 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 382 1 2 1 3.2 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
CHEMBL3654197 133567 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 382 1 2 1 3.2 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cc(F)cc3F)c2C1 nan
60152965 133569 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cccc3F)c2C1 nan
CHEMBL3654199 133569 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3c(F)cccc3F)c2C1 nan
50923586 131938 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL3644535 131938 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3c(F)cccc3F)c2c1 nan
60150904 133580 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3cc(F)c(F)cc3F)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654210 133580 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 392 1 2 1 3.2 NC(N)=NC(=O)N1Cc2c(-c3cc(F)c(F)cc3F)ccc(F)c2C2(CC2)C1 nan
67961424 131928 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2ncc(Cl)c(-c3ccc(F)cc3F)c2c1 nan
CHEMBL3644525 131928 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2ncc(Cl)c(-c3ccc(F)cc3F)c2c1 nan
50923580 131933 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 358 2 2 2 3.0 Cc1cnc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
CHEMBL3644530 131933 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 358 2 2 2 3.0 Cc1cnc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
44456033 162346 3 None 1 8 Rat 8.9 pKi = 8.9 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404372 162346 3 None 1 8 Rat 8.9 pKi = 8.9 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
50923443 131931 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 344 2 2 2 2.7 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL3644528 131931 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 344 2 2 2 2.7 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL5093295 222200 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Clc1ccc(CNC[C@H]2CCn3ccnc3C2)c2ncccc12 10.1021/acs.jmedchem.1c02031
91819723 133577 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 362 1 2 1 3.1 CC1CN(C(=O)N=C(N)N)Cc2c(-c3c(F)cccc3F)ccc(F)c21 nan
CHEMBL3654207 133577 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 362 1 2 1 3.1 CC1CN(C(=O)N=C(N)N)Cc2c(-c3c(F)cccc3F)ccc(F)c21 nan
50923442 131930 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3Cl)c2c1 nan
CHEMBL3644527 131930 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cccc3Cl)c2c1 nan
44456033 162346 3 None -1 8 Human 8.8 pKi = 8.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404372 162346 3 None -1 8 Human 8.8 pKi = 8.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
50923723 131943 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 322 2 2 2 2.8 Cc1cnc(-c2ccccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
CHEMBL3644540 131943 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 322 2 2 2 2.8 Cc1cnc(-c2ccccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
136152971 102132 0 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL256694 102132 0 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
60150901 133575 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 381 1 2 2 2.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3Cl)c2C1 nan
CHEMBL3654205 133575 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 381 1 2 2 2.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3Cl)c2C1 nan
50923720 131940 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 340 2 2 2 2.9 Cc1cnc(-c2c(F)cccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
CHEMBL3644537 131940 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 340 2 2 2 2.9 Cc1cnc(-c2c(F)cccc2F)c2cc(C(=O)N=C(N)N)ccc12 nan
16006607 102447 4 None -10 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 219 2 2 4 2.1 CC(C)Oc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
CHEMBL258075 102447 4 None -10 5 Human 8.0 pKi = 8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 219 2 2 4 2.1 CC(C)Oc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
135458393 162375 4 None 2 5 Human 8.0 pKi = 8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404511 162375 4 None 2 5 Human 8.0 pKi = 8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
135458392 104201 5 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL269964 104201 5 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
135458392 104201 5 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL269964 104201 5 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 0 2 3 2.2 CNC1=Nc2cccc(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
4106 9280 22 None -14 33 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
5358812 9280 22 None -14 33 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
89 9280 22 None -14 33 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL93240 9280 22 None -14 33 Human 7.0 pKi = 7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm030030n
CHEMBL5285512 201078 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 327 2 1 3 4.9 COc1ccc2[nH]c3c(-c4cn(C)c5ccccc45)nccc3c2c1 10.1021/acs.jmedchem.0c01887
44351139 25616 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128099 25616 0 None -1 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
44351140 25813 0 None -3 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128848 25813 0 None -3 3 Human 7.0 pKi = 7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
1220 6975 55 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
31 6975 55 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
7 6975 55 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
CHEMBL56 6975 55 None -1548 44 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
22857296 35923 0 None -123 4 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL13816 35923 0 None -123 4 Human 6.0 pKi = 6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL5083607 221652 0 None -83 9 Human 6.0 pKi = 6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCN(C)C2)ccc1Cl 10.1021/acs.jmedchem.1c00110
242 7258 124 None -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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 -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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 -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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 -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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 -144 51 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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
2389 10104 118 None -346 66 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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 -346 66 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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 -346 66 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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 -346 66 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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 -346 66 Human 6.0 pKi = 6 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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
135398737 7745 93 None -173 90 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
38 7745 93 None -173 90 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
722 7745 93 None -173 90 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
CHEMBL42 7745 93 None -173 90 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
DB00363 7745 93 None -173 90 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030030n
44397431 18529 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181632 18529 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL186261 18529 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 567 11 1 5 7.0 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCc3ccc4c(c3)OCO4)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
33630 185736 99 None -13 28 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells 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]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells 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
135514796 99833 0 None 2 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 226 1 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442270 99833 0 None 2 3 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 226 1 4 2 1.2 N=C1NC(=O)/C(=C\c2c[nH]c3ccccc23)N1 10.1016/j.bmc.2013.09.011
136152962 104696 1 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 175 0 2 3 1.6 CNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL272517 104696 1 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 175 0 2 3 1.6 CNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
49756 211091 13 None -138 8 Human 5.0 pKi = 5.0 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
CHEMBL7143 211091 13 None -138 8 Human 5.0 pKi = 5.0 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 232 4 1 2 2.6 COc1ccc2[nH]c(C)c(CCN(C)C)c2c1 10.1021/jm990550b
CHEMBL4520788 220754 10 None -48 25 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR5ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR5A
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
CHEMBL5078567 221344 1 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)C1(CNCc2ccc(Cl)c3cccnc23)CC1 10.1021/acs.jmedchem.1c02031
11088692 24846 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 326 7 0 3 4.2 CN(CCCOc1ccc(F)cc1)Cc1cn(C)c2ccccc12 10.1021/jm030080s
CHEMBL126666 24846 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 326 7 0 3 4.2 CN(CCCOc1ccc(F)cc1)Cc1cn(C)c2ccccc12 10.1021/jm030080s
5 6927 72 None -323 53 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 6927 72 None -323 53 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 6927 72 None -323 53 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 6927 72 None -323 53 Human 7.0 pKi = 7.0 Binding
Displacement of radiolabeled serotonin from human 5HT5A receptorDisplacement of radiolabeled serotonin from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
44351116 24722 1 None 1 2 Mouse 6.0 pKi = 6.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
CHEMBL126021 24722 1 None 1 2 Mouse 6.0 pKi = 6.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
136118729 99837 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442274 99837 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
44351116 24722 1 None -1 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
CHEMBL126021 24722 1 None -1 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 244 3 1 3 1.9 Cn1c2c(c3ccccc31)CN(CCCO)CC2 10.1021/jm030080s
135367857 171383 0 None -69 8 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4215875 171383 0 None -69 8 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 228 1 1 3 2.3 Cc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
71918568 126332 4 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
CHEMBL3459329 126332 4 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
44351511 26154 0 None -1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 5 0 3 4.3 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL129230 26154 0 None -1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 5 0 3 4.3 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccc(F)cc1)CC2 10.1021/jm030080s
44455980 20754 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL1196896 20754 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL558579 20754 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 0 2 3 1.5 CC1(C)NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
72550642 120855 0 None -134 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326982 120855 0 None -134 8 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
71918568 126332 4 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
CHEMBL3459329 126332 4 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL 317 7 2 3 3.0 O=C(CCCNCc1ccc(Cl)c2cccnc12)NC1CC1 10.1021/acs.jmedchem.1c02031
CHEMBL5074821 221115 1 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnn(C[C@H](C)NCc2cccc(OCc3ccccn3)c2)c1 10.1021/acs.jmedchem.1c02031
CHEMBL5087322 221864 6 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnc(NCc2ccccc2-n2ccnc2)nc1N(C)C 10.1021/acs.jmedchem.1c02031
CHEMBL5092728 222163 1 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CC(C)(C)c1ccc2c(c1)CN(C[C@@H](O)COC1CCOCC1)CC2 10.1021/acs.jmedchem.1c02031
CHEMBL5093652 222216 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None N#CC1(c2ccccc2)CCC(NCCc2nnc3ccccn23)CC1 10.1021/acs.jmedchem.1c02031
44397618 74396 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL190382 74396 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL5081379 221525 0 None -18 9 Human 6.9 pKi = 6.9 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44351102 23784 0 None 1 3 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL125417 23784 0 None 1 3 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
9817810 24144 1 None -501 8 Rat 5.9 pKi = 5.9 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL125745 24144 1 None -501 8 Rat 5.9 pKi = 5.9 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
44455963 161965 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 215 1 2 3 2.5 CC1NC(NC2CCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL402400 161965 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 215 1 2 3 2.5 CC1NC(NC2CCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44351183 25632 0 None -5 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
CHEMBL128184 25632 0 None -5 3 Mouse 5.9 pKi = 5.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
117209962 191648 1 None -46 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4852622 191648 1 None -46 7 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
136118716 99834 0 None 3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442271 99834 0 None 3 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
135367820 171600 0 None -23 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
CHEMBL4218672 171600 0 None -23 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from human 5-HT5A receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method
ChEMBL 232 1 1 3 2.2 Fc1ccc(-c2noc3c2CCNCC3)cc1 10.1021/acs.jmedchem.8b00642
136152965 102271 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 271 3 2 3 3.9 CC1NC(NCCC2CCCCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL257302 102271 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 271 3 2 3 3.9 CC1NC(NCCC2CCCCC2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
11443218 74252 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3ccc(CNC4CCN(Cc5ccccc5)CC4)cc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL189262 74252 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3ccc(CNC4CCN(Cc5ccccc5)CC4)cc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
24865725 194863 0 None -2511 12 Human 5.9 pKi = 5.9 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL497963 194863 0 None -2511 12 Human 5.9 pKi = 5.9 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
5 6927 72 None -323 53 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 6927 72 None -323 53 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 6927 72 None -323 53 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 6927 72 None -323 53 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
136118613 99838 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442275 99838 0 None -5 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL5087322 221864 6 None - 1 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnc(NCc2ccccc2-n2ccnc2)nc1N(C)C 10.1021/acs.jmedchem.1c02031
50923441 131927 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 358 2 2 2 3.0 Cc1cc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc2n1 nan
CHEMBL3644524 131927 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 358 2 2 2 3.0 Cc1cc(-c2c(F)cc(F)cc2F)c2cc(C(=O)N=C(N)N)ccc2n1 nan
11121216 36912 0 None -6 14 Human 7.9 pKi = 7.9 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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 -6 14 Human 7.9 pKi = 7.9 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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
10382508 214644 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
CHEMBL96504 214644 0 None -2 3 Human 7.9 pKi = 7.9 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
10382508 214644 0 None 2 3 Mouse 7.9 pKi = 7.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL96504 214644 0 None 2 3 Mouse 7.9 pKi = 7.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
44351059 26201 0 None - 1 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 0 2 4.6 Cn1c2c(c3ccccc31)CN(CCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL129472 26201 0 None - 1 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 0 2 4.6 Cn1c2c(c3ccccc31)CN(CCCCc1ccccc1)CC2 10.1021/jm030080s
5 6927 72 None -323 53 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
5202 6927 72 None -323 53 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
CHEMBL39 6927 72 None -323 53 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
DB08839 6927 72 None -323 53 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]LSD from human recombinant 5-HT5a receptor in HEK293 cells after 120 mins by scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/acs.jmedchem.6b01422
136118732 83021 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
CHEMBL2058409 83021 0 None 1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)NC(=O)/C1=C\c1c[nH]c2c(Br)cccc12 10.1016/j.bmc.2013.09.011
44351342 26203 0 None 1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
CHEMBL129476 26203 0 None 1 2 Mouse 6.9 pKi = 6.9 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
44456251 19608 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1188516 19608 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL536561 19608 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
44351183 25632 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
CHEMBL128184 25632 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1cccc2c3c(n(C)c12)CCN(CCCOc1ccc(F)cc1)C3 10.1021/jm030080s
1043 8363 14 None -169 29 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmc.2011.08.033
149 8363 14 None -169 29 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmc.2011.08.033
8223 8363 14 None -169 29 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmc.2011.08.033
CHEMBL442 8363 14 None -169 29 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmc.2011.08.033
DB00696 8363 14 None -169 29 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmc.2011.08.033
854531 159773 30 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 244 1 1 1 4.4 c1ccc(-c2nccc3c2[nH]c2ccccc23)cc1 10.1021/acs.jmedchem.0c01887
CHEMBL3975325 159773 30 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 244 1 1 1 4.4 c1ccc(-c2nccc3c2[nH]c2ccccc23)cc1 10.1021/acs.jmedchem.0c01887
136118619 83026 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058418 83026 0 None -2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
44456487 19645 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL1188759 19645 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL537248 19645 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1CNC(N)=N2 10.1016/j.bmcl.2007.10.080
136118616 83023 0 None -14 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058415 83023 0 None -14 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.3 C/N=C1\NC(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
136152963 104231 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL270131 104231 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
9888494 104947 0 None -660 13 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human 5-HT5A receptor was determinedBinding affinity towards cloned human 5-HT5A 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 -660 13 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human 5-HT5A receptor was determinedBinding affinity towards cloned human 5-HT5A 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
1043 8363 14 None -169 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
149 8363 14 None -169 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
8223 8363 14 None -169 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
CHEMBL442 8363 14 None -169 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
DB00696 8363 14 None -169 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
5 6927 72 None -891 53 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 6927 72 None -891 53 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 6927 72 None -891 53 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 6927 72 None -891 53 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL5280298 200838 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 294 1 1 1 5.5 c1ccc2cc(-c3nccc4c3[nH]c3ccccc34)ccc2c1 10.1021/acs.jmedchem.0c01887
53381002 72239 0 None -17 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 240 2 2 4 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12 10.1016/j.bmc.2011.08.033
CHEMBL1829959 72239 0 None -17 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
ChEMBL 240 2 2 4 2.2 COc1cccc2[nH]cc(-c3ccnc(N)n3)c12 10.1016/j.bmc.2011.08.033
136152981 104343 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 203 2 2 3 2.3 CCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL270658 104343 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 203 2 2 3 2.3 CCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
136118615 99840 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442277 99840 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3c(Br)cccc23)C1=O 10.1016/j.bmc.2013.09.011
44582676 196558 0 None -12 17 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A 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 -12 17 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A 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
24865727 199892 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL522708 199892 0 None -1000 11 Human 5.8 pKi = 5.8 Binding
Displacement of radioligand from human cloned 5HT5A receptorDisplacement of radioligand from human cloned 5HT5A receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
10947658 35475 0 None -14 16 Human 7.8 pKi = 7.8 Binding
Binding affinities against 5-hydroxytryptamine 5A receptorBinding affinities against 5-hydroxytryptamine 5A receptor
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 -14 16 Human 7.8 pKi = 7.8 Binding
Binding affinities against 5-hydroxytryptamine 5A receptorBinding affinities against 5-hydroxytryptamine 5A receptor
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
1043 8363 14 None -169 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
149 8363 14 None -169 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
8223 8363 14 None -169 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
CHEMBL442 8363 14 None -169 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
DB00696 8363 14 None -169 29 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
9867475 24785 0 None -524 9 Rat 5.8 pKi = 5.8 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126340 24785 0 None -524 9 Rat 5.8 pKi = 5.8 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
108182 10903 22 None -51 17 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1021/jm030030n
245 10903 22 None -51 17 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1021/jm030030n
CHEMBL18041 10903 22 None -51 17 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl 10.1021/jm030030n
CHEMBL4802043 220836 11 None - 1 Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CCOc1ccc(S(=O)(=O)Nc2ccc(Cl)cc2C#Cc2cnc(C(=O)O)cc2OC)c2ncccc12 10.6019/CHEMBL4800726
CHEMBL4802043 220836 11 None - 1 Human 5.8 pKi = 5.8 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CCOc1ccc(S(=O)(=O)Nc2ccc(Cl)cc2C#Cc2cnc(C(=O)O)cc2OC)c2ncccc12 10.6019/CHEMBL4800726
136152968 162103 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 245 2 2 4 2.1 CC1NC(NC[C@H]2CCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL403102 162103 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 245 2 2 4 2.1 CC1NC(NC[C@H]2CCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44351184 25633 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
CHEMBL128185 25633 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
10028436 10305 5 None -87 12 Human 6.8 pKi = 6.8 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptorBinding affinity towards 5-hydroxytryptamine 5A receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1021/jm030030n
3237 10305 5 None -87 12 Human 6.8 pKi = 6.8 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptorBinding affinity towards 5-hydroxytryptamine 5A receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1021/jm030030n
CHEMBL95104 10305 5 None -87 12 Human 6.8 pKi = 6.8 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptorBinding affinity towards 5-hydroxytryptamine 5A receptor
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1021/jm030030n
44351342 26203 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
CHEMBL129476 26203 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 5 0 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(=O)c1ccccc1)CC2 10.1021/jm030080s
6604756 105607 18 None -28 7 Human 6.8 pKi = 6.8 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
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 -28 7 Human 6.8 pKi = 6.8 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 275 6 0 2 4.2 CCCN(CCC)[C@@H]1CCc2c(OC)cccc2[C@@H]1C 10.1016/S0960-894X(01)80181-5
44582705 193775 0 None -10 13 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A 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 -10 13 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A 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
13972207 126395 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL34652 126395 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
10334023 119659 5 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 283 1 2 1 4.9 c1ccc2c(-c3nccc4c3[nH]c3ccccc34)c[nH]c2c1 10.1021/acs.jmedchem.0c01887
CHEMBL3309924 119659 5 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 283 1 2 1 4.9 c1ccc2c(-c3nccc4c3[nH]c3ccccc34)c[nH]c2c1 10.1021/acs.jmedchem.0c01887
CHEMBL5268604 200353 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 299 1 3 2 4.6 Oc1ccc2[nH]c3c(-c4c[nH]c5ccccc45)nccc3c2c1 10.1021/acs.jmedchem.0c01887
5 6927 72 None -323 53 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
5202 6927 72 None -323 53 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
CHEMBL39 6927 72 None -323 53 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
DB08839 6927 72 None -323 53 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
71459269 89735 0 None -7413 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
CHEMBL2181166 89735 0 None -7413 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 555 7 0 4 6.3 Fc1cccc2c1nc(OCC1CCN(CCCc3ccc(I)cc3)CC1)c1cccnc12 10.1021/jm300943r
44351063 26238 0 None 1 2 Mouse 5.8 pKi = 5.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL129774 26238 0 None 1 2 Mouse 5.8 pKi = 5.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
44351102 23784 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL125417 23784 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 332 6 0 2 4.9 Cn1c2c(c3ccccc31)CN(CCCCCc1ccccc1)CC2 10.1021/jm030080s
132060776 169181 0 None -5 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
CHEMBL4165863 169181 0 None -5 16 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 419 4 0 4 4.4 O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1 10.1016/j.ejmech.2018.02.024
136152974 102001 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCOCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL256049 102001 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCOCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
168268877 196749 0 None -38 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A 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 -38 12 Human 6.8 pKi = 6.8 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A 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
44351063 26238 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL129774 26238 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 328 3 0 2 4.2 Cn1c2c(c3ccccc31)CN(CC#CCCc1ccccc1)CC2 10.1021/jm030080s
25107716 9130 43 None -309 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
8436 9130 43 None -309 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
CHEMBL522691 9130 43 None -309 7 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 466 10 1 4 5.2 N#Cc1ccc(cc1)CNC(=O)CCCCCN1CCN(CC1)c1ccccc1c1ccccc1 10.1039/C8MD00313K
136100333 101290 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 CNC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL25163 101290 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 CNC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536557 101290 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 CNC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
44351193 123630 0 None 1 3 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338095 123630 0 None 1 3 Mouse 6.8 pKi = 6.8 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL5074880 221118 0 None -186 9 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
10028436 10305 5 None -87 12 Human 6.7 pKi = 6.7 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 10305 5 None -87 12 Human 6.7 pKi = 6.7 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 10305 5 None -87 12 Human 6.7 pKi = 6.7 Binding
Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )Compound was tested for its binding affinity in 5-hydroxytryptamine 5A receptor (using human cloned receptors in HEK 293 and [3H]5-CTas a radioligand )
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
136118728 99836 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442273 99836 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1 10.1016/j.bmc.2013.09.011
44351100 178250 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL446356 178250 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
44355204 28672 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
CHEMBL132019 28672 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
136152980 162058 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 217 3 2 3 2.7 CCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL402874 162058 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 217 3 2 3 2.7 CCCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
11035049 175357 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 335 5 1 4 3.6 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(N)cc1)CC2 10.1021/jm030080s
CHEMBL435814 175357 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 335 5 1 4 3.6 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(N)cc1)CC2 10.1021/jm030080s
10924201 124943 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 288 5 0 3 3.0 Cn1ccc2c1CCN(CCCOc1ccc(F)cc1)C2 10.1021/jm030080s
CHEMBL340861 124943 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 288 5 0 3 3.0 Cn1ccc2c1CCN(CCCOc1ccc(F)cc1)C2 10.1021/jm030080s
136179599 19631 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL1188681 19631 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL537022 19631 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 189 1 2 3 1.9 CCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
75306277 116031 0 None -99 23 Human 6.7 pKi = 6.7 Binding
Binding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A 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 serotonin 5-HT5A receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
11168912 18142 1 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1179769 18142 1 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL99071 18142 1 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 555 11 1 5 6.7 O=C(c1ccc2c(c1)OCO2)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
44397486 73886 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3cccc(CNC4CCN(Cc5ccccc5)CC4)c3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL187415 73886 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 489 11 2 3 6.4 c1ccc(CCNCc2ccc(-c3cccc(CNC4CCN(Cc5ccccc5)CC4)c3)cc2)cc1 10.1016/j.bmcl.2005.06.024
44456170 19923 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1190707 19923 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL541394 19923 1 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2c(F)cccc2CN1 10.1016/j.bmcl.2007.10.080
155536080 178893 0 None -13 10 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
CHEMBL4472703 178893 0 None -13 10 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting method
ChEMBL 219 2 1 2 2.9 CC[C@H]1c2cc(OC)ccc2CC[C@@]1(C)N 10.1021/acsmedchemlett.9b00225
10171 6845 18 None 5 6 Mouse 8.7 pKi = 8.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
272 6845 18 None 5 6 Mouse 8.7 pKi = 8.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
CHEMBL274384 6845 18 None 5 6 Mouse 8.7 pKi = 8.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 401 3 1 2 3.7 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)CC 10.1021/jm030030n
16093484 104836 6 None 3 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL273170 104836 6 None 3 6 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
50923724 131944 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3ccc(F)cc3F)c2c1 nan
CHEMBL3644541 131944 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(Cl)cnc(-c3ccc(F)cc3F)c2c1 nan
CHEMBL5079273 221390 4 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Clc1ccc(CNCCc2cccnc2)c2ncccc12 10.1021/acs.jmedchem.1c02031
91819722 133574 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cncc3F)c2C1 nan
CHEMBL3654204 133574 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3c(F)cncc3F)c2C1 nan
13972256 126396 1 None 1 2 Rat 8.6 pKi = 8.6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
CHEMBL34653 126396 1 None 1 2 Rat 8.6 pKi = 8.6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
91819720 133570 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 364 1 2 1 3.0 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3ccc(F)cc3F)c2C1 nan
CHEMBL3654200 133570 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 364 1 2 1 3.0 NC(N)=NC(=O)N1CCc2c(Cl)ccc(-c3ccc(F)cc3F)c2C1 nan
60150905 133579 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 302 1 2 1 1.9 NC(N)=NC(=O)N1Cc2c(C3CC3)ccc(F)c2C2(CC2)C1 nan
CHEMBL3654209 133579 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 302 1 2 1 1.9 NC(N)=NC(=O)N1Cc2c(C3CC3)ccc(F)c2C2(CC2)C1 nan
136152964 201718 0 None 2 8 Rat 8.5 pKi = 8.5 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL541993 201718 0 None 2 8 Rat 8.5 pKi = 8.5 Binding
Binding affinity to rat 5HT5A receptorBinding affinity to rat 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
1809 6922 32 None -229 37 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
4 6922 32 None -229 37 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
CHEMBL18840 6922 32 None -229 37 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
1809 6922 32 None -229 37 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
4 6922 32 None -229 37 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
CHEMBL18840 6922 32 None -229 37 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm030030n
44327952 214823 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
CHEMBL97518 214823 0 None -3 5 Human 6.7 pKi = 6.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
10872812 24885 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 388 5 0 3 5.3 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)c(Cl)c1)CC2 10.1021/jm030080s
CHEMBL126897 24885 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 388 5 0 3 5.3 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)c(Cl)c1)CC2 10.1021/jm030080s
10882775 24886 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 354 5 0 3 4.7 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)cc1)CC2 10.1021/jm030080s
CHEMBL126898 24886 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 354 5 0 3 4.7 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(Cl)cc1)CC2 10.1021/jm030080s
1524 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
197 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
3822 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
88 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
CHEMBL51 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
DB12465 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
1524 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
197 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
3822 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
88 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
CHEMBL51 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
DB12465 8962 96 None -1862 51 Human 4.7 pKi = 4.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm030030n
71452650 85271 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL2111848 85271 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL5082151 221567 1 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)CCNCc1ccc(Cl)c2cccnc12 10.1021/acs.jmedchem.1c02031
127036932 144126 0 None -69 22 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 144126 0 None -69 22 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL5074821 221115 1 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Cc1cnn(C[C@H](C)NCc2cccc(OCc3ccccn3)c2)c1 10.1021/acs.jmedchem.1c02031
2760172 105585 32 None 1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 c1ccc2cc(N3CCNCC3)ccc2c1 10.1021/jm030030n
CHEMBL278509 105585 32 None 1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 c1ccc2cc(N3CCNCC3)ccc2c1 10.1021/jm030030n
CHEMBL5084249 221684 0 None -251 8 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCN(CC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
73346042 98609 5 None -21379 17 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A 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 -21379 17 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A 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
CHEMBL5092728 222163 1 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CC(C)(C)c1ccc2c(c1)CN(C[C@@H](O)COC1CCOCC1)CC2 10.1021/acs.jmedchem.1c02031
70530 103732 104 None -6 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 178 1 2 3 0.8 Oc1ccccc1N1CCNCC1 10.1021/jm030030n
CHEMBL266250 103732 104 None -6 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 178 1 2 3 0.8 Oc1ccccc1N1CCNCC1 10.1021/jm030030n
1043 8363 14 None -169 29 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm990550b
149 8363 14 None -169 29 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm990550b
8223 8363 14 None -169 29 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm990550b
CHEMBL442 8363 14 None -169 29 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm990550b
DB00696 8363 14 None -169 29 Human 7.7 pKi = 7.7 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm990550b
136152966 102368 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 289 3 2 4 2.9 COc1c(Cl)ccc2c1C(C)NC(NCC(F)F)=N2 10.1016/j.bmcl.2007.10.078
CHEMBL257744 102368 0 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 289 3 2 4 2.9 COc1c(Cl)ccc2c1C(C)NC(NCC(F)F)=N2 10.1016/j.bmcl.2007.10.078
135458427 178332 0 None -5 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 283 4 2 4 3.0 CC(C)Oc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
CHEMBL446459 178332 0 None -5 5 Human 7.7 pKi = 7.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 283 4 2 4 3.0 CC(C)Oc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
44456395 102446 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 225 1 2 4 2.0 COc1c(Cl)ccc2c1C(C)NC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL258073 102446 0 None -1 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 225 1 2 4 2.0 COc1c(Cl)ccc2c1C(C)NC(N)=N2 10.1016/j.bmcl.2007.10.080
134138168 154469 0 None -19 10 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 154469 0 None -19 10 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
4806 10780 88 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 10780 88 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 10780 88 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 10780 88 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 10780 88 None -10 13 Human 6.7 pKi = 6.7 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
24841480 190678 0 None -1096 20 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 190678 0 None -1096 20 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT5A receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
181743 185351 5 None -1122 22 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A 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 -1122 22 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]LSD from human 5HT5A receptorDisplacement of [3H]LSD from human 5HT5A receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL4576555 220796 5 None -2 19 Human 5.7 pKi = 5.7 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
44351180 24856 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126737 24856 0 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
44351077 123748 0 None 1 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338696 123748 0 None 1 3 Mouse 6.7 pKi = 6.7 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
118464420 145023 0 None -38 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
CHEMBL3770342 145023 0 None -38 8 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 335 1 3 5 2.8 NC1=NC2(CCCCC2)NC(Nc2cccc(Br)c2)=N1 10.1021/acs.jmedchem.5b01631
10324985 83556 8 None -169 17 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A 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 -169 17 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A 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 -169 17 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
168293874 198958 0 None -52 11 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A 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 -52 11 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A 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
CHEMBL5090584 222050 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)CCNCc1cccc2cccnc12 10.1021/acs.jmedchem.1c02031
CHEMBL5071978 221051 0 None -3 6 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCN(CC)Cc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
117209858 191333 1 None -147 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4848305 191333 1 None -147 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
122334 7110 23 None -51 7 Human 5.6 pKi = 5.6 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
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 -51 7 Human 5.6 pKi = 5.6 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
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 -51 7 Human 5.6 pKi = 5.6 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
ChEMBL 233 4 1 2 3.1 CCCN[C@@H]1CCc2c([C@@H]1C)cccc2OC 10.1016/S0960-894X(01)80181-5
136118614 99839 0 None -25 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2442276 99839 0 None -25 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
155770281 184526 0 None -2 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A (unknown origin)Binding affinity to 5HT5A (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4642592 184526 0 None -2 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A (unknown origin)Binding affinity to 5HT5A (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
44355141 31418 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL134331 31418 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
127036953 144293 0 None -239 22 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 144293 0 None -239 22 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
44455986 104372 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 1 2 3 1.7 CCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL270841 104372 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 1 2 3 1.7 CCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL5093342 222343 0 None -28 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095971 222343 0 None -28 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5090884 222356 0 None -37 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096072 222356 0 None -37 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
136152973 102000 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCCOCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
CHEMBL256048 102000 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 247 5 2 4 2.4 CCCOCCNC1=Nc2ccccc2C(C)N1 10.1016/j.bmcl.2007.10.078
107838 104098 112 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030030n
CHEMBL269236 104098 112 None 1 2 Mouse 5.6 pKi = 5.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptorBinding affinity towards mouse 5-hydroxytryptamine 5A receptor
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030030n
CHEMBL4576555 220796 5 None -2 19 Human 5.6 pKi = 5.6 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
CHEMBL4576555 220796 5 None -2 19 Human 5.6 pKi = 5.6 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a HTR5ASelectivity interaction (GPCR panel (PDSP screen)) EUB0000705a HTR5A
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL5212743
44351140 25813 0 None 3 3 Mouse 7.6 pKi = 7.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128848 25813 0 None 3 3 Mouse 7.6 pKi = 7.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
11444050 18526 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1 10.1016/j.bmcl.2005.06.024
CHEMBL1181620 18526 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1 10.1016/j.bmcl.2005.06.024
CHEMBL185676 18526 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 537 13 2 3 7.1 O=C(CCC1CCCC1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)CC1CCCCN1 10.1016/j.bmcl.2005.06.024
9827938 18543 0 None 6 12 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
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 6 12 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
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 6 12 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
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
11352884 73932 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL187621 73932 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
135966709 161934 4 None -10 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 233 2 2 4 2.3 CNC1=Nc2c(OC(C)C)cccc2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL402179 161934 4 None -10 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 233 2 2 4 2.3 CNC1=Nc2c(OC(C)C)cccc2C(C)N1 10.1016/j.bmcl.2007.10.080
5 6927 72 None -323 53 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
5202 6927 72 None -323 53 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
CHEMBL39 6927 72 None -323 53 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
DB08839 6927 72 None -323 53 Human 6.6 pKi = 6.6 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm030030n
10893866 27080 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 6 0 5 3.9 Cn1c2c(c3ccccc31)CN(CCCOc1ccc([N+](=O)[O-])cc1)CC2 10.1021/jm030080s
CHEMBL130585 27080 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 6 0 5 3.9 Cn1c2c(c3ccccc31)CN(CCCOc1ccc([N+](=O)[O-])cc1)CC2 10.1021/jm030080s
44351099 24827 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 304 4 0 2 4.2 Cn1c2c(c3ccccc31)CN(CCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL126574 24827 0 None - 1 Mouse 6.6 pKi = 6.6 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 304 4 0 2 4.2 Cn1c2c(c3ccccc31)CN(CCCc1ccccc1)CC2 10.1021/jm030080s
1220 6975 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
31 6975 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
7 6975 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
CHEMBL56 6975 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
1220 6975 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
31 6975 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
7 6975 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
CHEMBL56 6975 55 None -1548 44 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm030030n
44397593 18541 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181677 18541 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188440 18541 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 553 14 1 4 6.1 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)S(=O)(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
44397513 19038 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1184719 19038 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL365422 19038 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 523 12 1 3 6.5 CN(C)CCN(Cc1ccc(-c2ccc(CNC3Cc4ccccc4C3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
44455943 175781 5 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 243 1 2 3 3.0 CCC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL439240 175781 5 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 243 1 2 3 3.0 CCC1NC(N)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.080
10472143 126055 0 None -60 16 Human 7.6 pKi = 7.6 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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 -60 16 Human 7.6 pKi = 7.6 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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
44351193 123630 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338095 123630 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cc(Cl)ccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL5092524 222154 2 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN(C)S(=O)(=O)CCNCc1ccc(F)c2cccnc12 10.1021/acs.jmedchem.1c02031
44456284 19617 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1188595 19617 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL536789 19617 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)N=C(N)NC2 10.1016/j.bmcl.2007.10.080
136152969 162104 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 286 1 2 4 1.9 CC1NC(NC2CCCCN(C)C2=O)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL403103 162104 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 286 1 2 4 1.9 CC1NC(NC2CCCCN(C)C2=O)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
135458428 162313 0 None 1 5 Human 7.6 pKi = 7.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 255 3 2 4 2.2 COc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
CHEMBL404248 162313 0 None 1 5 Human 7.6 pKi = 7.6 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 255 3 2 4 2.2 COc1cccc2c1N=C(NCC(F)F)NC2C 10.1016/j.bmcl.2007.10.078
12683497 104296 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 0 1 3 1.3 CN(C)C1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL270409 104296 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 175 0 1 3 1.3 CN(C)C1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
4407909 199645 1 None -50 10 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5182943 199645 1 None -50 10 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5221893 199645 1 None -50 10 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 356 4 2 4 3.6 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(F)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
44351077 123748 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL338696 123748 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 352 5 1 3 4.2 Cn1c2c(c3ccccc31)CN(CCCC(O)c1ccc(F)cc1)CC2 10.1021/jm030080s
44374431 61726 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
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 -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
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
90469115 192621 4 None -954 17 Human 5.5 pKi = 5.5 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 192621 4 None -954 17 Human 5.5 pKi = 5.5 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL5093652 222216 2 None - 1 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None N#CC1(c2ccccc2)CCC(NCCc2nnc3ccccn23)CC1 10.1021/acs.jmedchem.1c02031
CHEMBL5094493 222278 0 None -144 7 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCN(CCC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44351171 123627 0 None 2 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL338081 123627 0 None 2 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOCc1ccccc1)CC2 10.1021/jm030080s
44275750 99988 39 None 1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 228 1 2 3 2.0 Oc1ccc2cccc(N3CCNCC3)c2c1 10.1021/jm030030n
CHEMBL24462 99988 39 None 1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 228 1 2 3 2.0 Oc1ccc2cccc(N3CCNCC3)c2c1 10.1021/jm030030n
CHEMBL5075486 221155 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=S1(=O)CCC[C@@H](CNCc2ccc(Cl)c3cccnc23)C1 10.1021/acs.jmedchem.1c02031
50923584 131936 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 326 2 2 2 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3F)c2c1 nan
CHEMBL3644533 131936 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 326 2 2 2 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3F)c2c1 nan
50923585 131937 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 342 2 2 2 3.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3Cl)c2c1 nan
CHEMBL3644534 131937 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 342 2 2 2 3.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccccc3Cl)c2c1 nan
91819719 133566 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2cccc(-c3cc(F)c(F)cc3F)c2C1 nan
CHEMBL3654196 133566 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 348 1 2 1 2.5 NC(N)=NC(=O)N1CCc2cccc(-c3cc(F)c(F)cc3F)c2C1 nan
60150903 133581 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3cc(F)c(F)cc3F)c2C1 nan
CHEMBL3654211 133581 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 366 1 2 1 2.7 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3cc(F)c(F)cc3F)c2C1 nan
50923581 131929 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 372 2 2 2 3.4 Cc1nc2ccc(C(=O)N=C(N)N)cc2c(-c2c(F)cc(F)cc2F)c1C nan
CHEMBL3644526 131929 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 372 2 2 2 3.4 Cc1nc2ccc(C(=O)N=C(N)N)cc2c(-c2c(F)cc(F)cc2F)c1C nan
60150900 133573 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 345 1 2 2 2.1 Cc1ccc(-c2ncc(F)cc2F)c2c1CCN(C(=O)N=C(N)N)C2 nan
CHEMBL3654203 133573 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 345 1 2 2 2.1 Cc1ccc(-c2ncc(F)cc2F)c2c1CCN(C(=O)N=C(N)N)C2 nan
24936155 101397 0 None -501 7 Human 5.5 pKi = 5.5 Binding
Inhibition of 5HT5A receptorInhibition of 5HT5A receptor
ChEMBL 508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 10.1016/j.bmcl.2007.10.109
CHEMBL252258 101397 0 None -501 7 Human 5.5 pKi = 5.5 Binding
Inhibition of 5HT5A receptorInhibition of 5HT5A receptor
ChEMBL 508 4 2 3 5.1 CC(=O)N1C2C=C(CN3C4CCC3CC(NC(=O)Nc3cc(F)cc(C(F)(F)F)c3)C4)CC1CCC2 10.1016/j.bmcl.2007.10.109
44374648 126750 0 None -18 4 Human 5.5 pKi = 5.5 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
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 -18 4 Human 5.5 pKi = 5.5 Binding
Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )Binding affinity was measured at cloned mammalian 5-HT1A receptor expressed in CHO-K1 cells (using [3H]8-OH-DPAT )
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
4106 9280 22 None -14 33 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
5358812 9280 22 None -14 33 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
89 9280 22 None -14 33 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
CHEMBL93240 9280 22 None -14 33 Human 7.5 pKi = 7.5 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/acs.jnatprod.0c00793
11272242 18534 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1181641 18534 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL186849 18534 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccn3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
11364267 74313 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL189689 74313 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 512 14 1 4 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)nc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
44355165 123248 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
CHEMBL336124 123248 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
10287730 10309 40 None -3981 12 Human 5.5 pKi = 5.5 Binding
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
77 10309 40 None -3981 12 Human 5.5 pKi = 5.5 Binding
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
CHEMBL425190 10309 40 None -3981 12 Human 5.5 pKi = 5.5 Binding
Binding affinity for human 5-hydroxytryptamine 5A receptor Binding affinity for human 5-hydroxytryptamine 5A receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
44397511 18540 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1181669 18540 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL188050 18540 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 407 10 1 3 4.7 CN(C)CCN(Cc1ccc(-c2ccc(CN)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
107838 104098 112 None -1 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030080s
CHEMBL269236 104098 112 None -1 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 172 0 2 1 1.8 c1ccc2c3c([nH]c2c1)CNCC3 10.1021/jm030080s
127036186 144192 0 None -102 19 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 144192 0 None -102 19 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
216239 30567 118 None -6 7 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1200485 30567 118 None -6 7 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
CHEMBL1336 30567 118 None -6 7 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1021/jm300338m
136116062 104456 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL271253 104456 0 None 2 4 Human 7.5 pKi = 7.5 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.078
71452650 85271 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL2111848 85271 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C\CCc1ccccc1)CC2 10.1021/jm030080s
50878551 97520 61 None -85 18 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 97520 61 None -85 18 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
136118651 83099 0 None -9 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058706 83099 0 None -9 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3c(Br)cccc23)N1 10.1016/j.bmc.2013.09.011
10892139 172366 0 None -1 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3c([nH]c4ccccc34)C2)cc1 10.1021/jm030080s
CHEMBL424258 172366 0 None -1 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3c([nH]c4ccccc34)C2)cc1 10.1021/jm030080s
122483275 144888 0 None -15 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764133 144888 0 None -15 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765875 144888 0 None -15 8 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 427 6 1 5 5.1 O=C(CCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
136118648 83096 0 None -67 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2058703 83096 0 None -67 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.0 C/N=C1\NC(=O)/C(=C/c2c[nH]c3cccc(Br)c23)N1 10.1016/j.bmc.2013.09.011
44351361 24740 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 5 1 4 4.3 Cn1c2c(c3ccccc31)CN(CCC/C(=N/O)c1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126138 24740 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 365 5 1 4 4.3 Cn1c2c(c3ccccc31)CN(CCC/C(=N/O)c1ccc(F)cc1)CC2 10.1021/jm030080s
9862256 213899 0 None -2238 9 Rat 5.5 pKi = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL92139 213899 0 None -2238 9 Rat 5.5 pKi = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
10035245 36467 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL13864 36467 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL538340 36467 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cc(Cl)ccc2CN1 10.1016/j.bmcl.2007.10.080
10926167 124871 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 6 0 4 4.0 COc1ccc(OCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
CHEMBL340646 124871 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 350 6 0 4 4.0 COc1ccc(OCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
44351100 178250 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL446356 178250 0 None -1 3 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 330 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(C/C=C/CCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL5094680 222289 0 None -23 8 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
11726973 24873 0 None 1 3 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
CHEMBL126823 24873 0 None 1 3 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
136152970 102131 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 309 2 2 5 2.8 CC1NC(NCC2COc3ccccc3O2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL256693 102131 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 309 2 2 5 2.8 CC1NC(NCC2COc3ccccc3O2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44355425 30360 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL133433 30360 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
44455985 19924 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL1190709 19924 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL541396 19924 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44455985 19924 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL1190709 19924 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL541396 19924 1 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.3 CC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL5074190 221093 0 None -151 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
44355426 30951 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
CHEMBL133935 30951 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
752521 205516 8 None -19 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
CHEMBL582877 205516 8 None -19 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
136152978 102301 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 207 2 2 3 1.9 CC1NC(NCCF)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL257450 102301 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 207 2 2 3 1.9 CC1NC(NCCF)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
44397435 18535 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181643 18535 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL187029 18535 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 506 12 2 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)Nc1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL5089996 222014 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None CN1CC[C@H](CNCc2ccc(Cl)c3cccnc23)CC1=O 10.1021/acs.jmedchem.1c02031
50923444 131932 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccc(F)cc3Cl)c2c1 nan
CHEMBL3644529 131932 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 360 2 2 2 3.2 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ccc(F)cc3Cl)c2c1 nan
91819724 133583 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 331 1 2 2 1.8 NC(N)=NC(=O)N1CCc2cccc(-c3ncc(F)cc3F)c2C1 nan
CHEMBL3654213 133583 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 331 1 2 2 1.8 NC(N)=NC(=O)N1CCc2cccc(-c3ncc(F)cc3F)c2C1 nan
91819718 133565 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3F)c2C1 nan
CHEMBL3654195 133565 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 365 1 2 2 2.4 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(Cl)cc3F)c2C1 nan
50923722 131942 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 376 3 2 2 3.5 NC(N)=NC(=O)c1ccc2c(C(F)F)cnc(-c3c(F)cccc3F)c2c1 nan
CHEMBL3644539 131942 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 376 3 2 2 3.5 NC(N)=NC(=O)c1ccc2c(C(F)F)cnc(-c3c(F)cccc3F)c2c1 nan
50923719 131939 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3Cl)c2c1 nan
CHEMBL3644536 131939 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3Cl)c2c1 nan
16093485 161842 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 239 1 2 4 2.3 COc1cc(Cl)c(C)c2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
CHEMBL401745 161842 0 None -1 5 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 239 1 2 4 2.3 COc1cc(Cl)c(C)c2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
13972211 145715 1 None 28 2 Rat 8.3 pKi = 8.3 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL37844 145715 1 None 28 2 Rat 8.3 pKi = 8.3 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 1 2 3.4 CCCN(CCC)[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
1342 6824 49 None -16 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
3 6824 49 None -16 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
CHEMBL277120 6824 49 None -16 19 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
1043 8363 14 None -169 29 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm030030n
149 8363 14 None -169 29 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm030030n
8223 8363 14 None -169 29 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm030030n
CHEMBL442 8363 14 None -169 29 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm030030n
DB00696 8363 14 None -169 29 Human 7.4 pKi = 7.4 Binding
Binding affinity for rodent 5-hydroxytryptamine 5A receptorBinding affinity for rodent 5-hydroxytryptamine 5A receptor
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1021/jm030030n
1342 6824 49 None -16 19 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
3 6824 49 None -16 19 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
CHEMBL277120 6824 49 None -16 19 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]- LSD as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm030030n
11808247 24847 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1021/jm030080s
CHEMBL126667 24847 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1021/jm030080s
CHEMBL3819366 24847 0 None -4 9 Human 6.4 pKi = 6.4 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligandBinding affinity towards 5-hydroxytryptamine 5A receptor using lysergic acid diethylamide (LSD) as radioligand
ChEMBL 285 5 0 2 3.7 Fc1ccc(OCCCN2CCc3ccccc3C2)cc1 10.1021/jm030080s
9927441 214173 0 None -1174 9 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
CHEMBL93868 214173 0 None -1174 9 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
44455962 176125 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL441896 176125 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 C[C@H]1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
145980271 173271 0 None -8 16 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells 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 -8 16 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells 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
92042876 158115 0 None -79 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 158115 0 None -79 10 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
127026052 144331 0 None -257 19 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 144331 0 None -257 19 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5-HT 5A (unknown origin) by competition binding assayBinding affinity to 5-HT 5A (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
9904281 54523 28 None 4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1548 54523 28 None 4 7 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 215 0 2 3 2.0 NC1=Nc2ccc(Cl)c(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
44355180 172113 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 0 2 3.1 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL423527 172113 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 233 6 0 2 3.1 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
44351101 23721 0 None 1 2 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 346 7 0 2 5.3 Cn1c2c(c3ccccc31)CN(CCCCCCc1ccccc1)CC2 10.1021/jm030080s
CHEMBL125361 23721 0 None 1 2 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 346 7 0 2 5.3 Cn1c2c(c3ccccc31)CN(CCCCCCc1ccccc1)CC2 10.1021/jm030080s
9796627 103428 0 None -154 7 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL263700 103428 0 None -154 7 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligandBinding affinity against 5-hydroxytryptamine 5A receptor in HEK 293 cells was determined using [3H]LSD as radioligand
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
3649661 144997 7 None -63 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770106 144997 7 None -63 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 329 3 3 7 2.2 CCOC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
12 8335 17 None -208 7 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
6918513 8335 17 None -208 7 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
CHEMBL267615 8335 17 None -208 7 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10.1021/jm990550b
44456246 19604 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1188440 19604 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL536335 19604 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
44456400 19606 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells 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 -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells 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 -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells 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 -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells 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
136118660 83031 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058428 83031 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cc(Br)ccc23)N1C 10.1016/j.bmc.2013.09.011
145963830 170902 0 None -46 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
CHEMBL4209942 170902 0 None -46 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 335 4 2 4 4.0 Oc1ccccc1C1=NC(Cc2c[nH]cn2)C(c2ccccc2)S1 10.1021/acs.jnatprod.7b00317
136152976 174250 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 243 1 2 3 2.5 CC1NC(NCC(F)(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL429925 174250 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 243 1 2 3 2.5 CC1NC(NCC(F)(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
145986752 174055 0 None -12 17 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells 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 -12 17 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells 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
122483281 144886 0 None 6 8 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3763779 144886 0 None 6 8 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765873 144886 0 None 6 8 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
16006492 104245 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL270177 104245 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
44397364 129938 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL361256 129938 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 518 13 1 4 5.7 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cn2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
16006492 104245 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270177 104245 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
16006492 104245 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270177 104245 7 None 3 6 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 195 0 2 3 2.0 CC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
50923582 131934 2 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 345 2 2 3 2.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3F)c2c1 nan
CHEMBL3644531 131934 2 None - 1 Human 8.3 pKi = 8.3 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 345 2 2 3 2.1 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3c(F)cncc3F)c2c1 nan
135458410 173968 0 None 3 6 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL429136 173968 0 None 3 6 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 CC1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
11191906 18539 0 None 6 12 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
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 6 12 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
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 6 12 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
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
4713248 214686 3 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
CHEMBL96729 214686 3 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
4713248 214686 3 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
CHEMBL96729 214686 3 None -5 3 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 281 5 2 3 1.2 CNS(=O)(=O)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm030030n
44397427 18528 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1 10.1016/j.bmcl.2005.06.024
CHEMBL1181625 18528 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1 10.1016/j.bmcl.2005.06.024
CHEMBL185996 18528 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 580 14 1 3 8.0 COc1cccc(CCN(Cc2ccc(-c3ccc(CNCCc4ccccc4)cc3)cc2)C(=O)/C=C/c2ccccc2)c1 10.1016/j.bmcl.2005.06.024
44456400 19606 0 None -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells 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 -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells 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 -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells 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 -2 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells after 90 mins by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in CHO cells 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
136152972 101999 0 None -2 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL256047 101999 0 None -2 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 293 2 2 3 3.5 C[C@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c21 10.1016/j.bmcl.2007.10.078
44355128 125260 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 219 5 1 2 2.8 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL341373 125260 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 219 5 1 2 2.8 CCN(CC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
136118658 83029 0 None -5 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058426 83029 0 None -5 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3cccc(Br)c23)N1C 10.1016/j.bmc.2013.09.011
379995 123629 2 None - 1 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 1 2 4.3 O=C(CCCN1CCc2[nH]c3ccccc3c2C1)c1ccc(F)cc1 10.1021/jm030080s
CHEMBL338091 123629 2 None - 1 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 1 2 4.3 O=C(CCCN1CCc2[nH]c3ccccc3c2C1)c1ccc(F)cc1 10.1021/jm030080s
CHEMBL4748908 220814 1 None -64 12 Human 5.3 pKi = 5.3 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
6918515 9390 38 None -158 7 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
71 9390 38 None -158 7 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
CHEMBL7318 9390 38 None -158 7 Human 5.3 pKi = 5.3 Binding
Compound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptorCompound was evaluated for its binding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10.1021/jm990550b
72550645 120866 0 None -72 8 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326993 120866 0 None -72 8 Human 6.3 pKi = 6.3 Binding
Binding affinity to 5-HT5A (unknown origin)Binding affinity to 5-HT5A (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
18677411 214023 11 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030080s
CHEMBL92879 214023 11 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030080s
18677411 214023 11 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030030n
CHEMBL92879 214023 11 None - 1 Mouse 5.3 pKi = 5.3 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 186 0 1 2 1.8 Cn1c2c(c3ccccc31)CNCC2 10.1021/jm030030n
135474338 196050 0 None -28 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL511879 196050 0 None -28 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 318 1 3 2 2.3 CN1C(=N)N/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
10382508 214644 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
CHEMBL96504 214644 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptorBinding affinity towards human 5-hydroxytryptamine 5A receptor
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030030n
10382508 214644 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL96504 214644 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 338 5 0 3 4.1 Cn1c2c(c3ccccc31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
11045379 26143 0 None -4 2 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 1 2 4.2 O=C(CCCN1CCc2c([nH]c3ccccc23)C1)c1ccccc1 10.1021/jm030080s
CHEMBL129163 26143 0 None -4 2 Mouse 6.3 pKi = 6.3 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 318 5 1 2 4.2 O=C(CCCN1CCc2c([nH]c3ccccc23)C1)c1ccccc1 10.1021/jm030080s
44456443 19763 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1189631 19763 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL539103 19763 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cccc(F)c2CN1 10.1016/j.bmcl.2007.10.080
16573 184398 34 None -28 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL464099 184398 34 None -28 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assayDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in Flp-In CHO cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL5085238 221737 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=S1(=O)CC[C@@H](CNCc2cccc3cccnc23)C1 10.1021/acs.jmedchem.1c02031
44355424 28798 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
CHEMBL132123 28798 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@@H]1C[C@@H]1c1cccc(O)c1 10.1016/0960-894X(96)00045-5
71462776 89738 0 None -4786 7 Human 5.2 pKi = 5.2 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
CHEMBL2181169 89738 0 None -4786 7 Human 5.2 pKi = 5.2 Binding
Binding affinity to human 5HT5A by Cerep protocol based assayBinding affinity to human 5HT5A by Cerep protocol based assay
ChEMBL 460 5 0 3 5.5 CCCN1CCC(COc2nc3c(I)cccc3c3ccccc23)CC1 10.1021/jm300943r
44351180 24856 0 None -2 3 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126737 24856 0 None -2 3 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 372 5 0 3 4.8 Cn1c2c(c3cccc(Cl)c31)CN(CCCOc1ccc(F)cc1)CC2 10.1021/jm030080s
118464425 145087 0 None -15 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 145087 0 None -15 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
50923721 131941 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ncc(F)cc3Cl)c2c1 nan
CHEMBL3644538 131941 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 361 2 2 3 2.6 NC(N)=NC(=O)c1ccc2c(F)cnc(-c3ncc(F)cc3Cl)c2c1 nan
135458394 104467 5 None 2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 243 0 2 3 2.9 CNC1=Nc2ccc(Cl)c(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
CHEMBL271298 104467 5 None 2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 243 0 2 3 2.9 CNC1=Nc2ccc(Cl)c(Cl)c2C(C)N1 10.1016/j.bmcl.2007.10.080
16006606 164440 3 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 191 1 2 4 1.3 COc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
CHEMBL408152 164440 3 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 191 1 2 4 1.3 COc1cccc2c1N=C(N)NC2C 10.1016/j.bmcl.2007.10.080
135458393 162375 4 None 2 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL404511 162375 4 None 2 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 CC1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
11168182 10307 25 None 50 13 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
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 50 13 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
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 50 13 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
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
16006605 104768 3 None -2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL272781 104768 3 None -2 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 229 0 2 3 2.6 CC1NC(N)=Nc2c(Cl)ccc(Cl)c21 10.1016/j.bmcl.2007.10.080
91819721 133572 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 382 1 2 1 3.5 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(Cl)c2C(F)C1 nan
CHEMBL3654202 133572 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 382 1 2 1 3.5 NC(N)=NC(=O)N1Cc2c(-c3ccc(F)cc3F)ccc(Cl)c2C(F)C1 nan
CHEMBL5093969 222240 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None Clc1ccc(CNCC[C@@H]2CCOC2)c2ncccc12 10.1021/acs.jmedchem.1c02031
CHEMBL5094012 222242 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=C1C[C@H](CNCc2ccc(Cl)c3cccnc23)CN1C1CC1 10.1021/acs.jmedchem.1c02031
136152964 201718 0 None -2 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
CHEMBL541993 201718 0 None -2 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 259 2 2 3 2.8 C[C@@H]1NC(NCC(F)F)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.078
60150899 133571 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 349 1 2 2 1.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(F)cc3F)c2C1 nan
CHEMBL3654201 133571 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).Binding Assay: A test compound and 150 uM of a DMSO solution of 5-carboxamide tryptamine (5-CT) were added to a 96-well plate at 2 ul/well and suspended in the incubation buffer, and the HEK293 cells forced to express the human 5-HT5A receptor that were prepared at a concentration of 200 ug/ml were added thereto at 100 ul/well. The cells were incubated for 15 minutes at room temperature, and then a [3H]5-CT solution (3 nM [3H]5-CT, incubation buffer) was added thereto at 100 ul/well.100 ul of the cell solution was separately dispensed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Thereafter, the radioactivity thereof was measured using a liquid scintillation counter. The cells were incubated for 60 minutes at 37 C. The reaction mixture was aspirated into a 96-well GF/C filter plate having undergone pretreatment with 0.2% polyethyleneimine, and washed 6 times with an ice-cold 50 mM Tris (pH 7.4).
ChEMBL 349 1 2 2 1.9 NC(N)=NC(=O)N1CCc2c(F)ccc(-c3ncc(F)cc3F)c2C1 nan
22980542 24803 0 None -3 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
CHEMBL126438 24803 0 None -3 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 306 5 1 2 4.0 c1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
73353884 99097 0 None -5 8 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL2429890 99097 0 None -5 8 Human 5.2 pKi = 5.2 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 295 3 1 3 2.7 c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2 10.1016/j.bmc.2013.07.045
CHEMBL4748908 220814 1 None -64 12 Human 5.2 pKi = 5.2 Binding
GPCRScan assay: inhibition of 5-HT5AGPCRScan assay: inhibition of 5-HT5A
ChEMBL None None None CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1 10.6019/CHEMBL4800732
11726973 24873 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
CHEMBL126823 24873 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 320 5 0 3 4.0 Cn1c2c(c3ccccc31)CCN(CCCOc1ccccc1)C2 10.1021/jm030080s
146025727 178464 0 None -229 27 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO 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 -229 27 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO 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
44327952 214823 0 None 1 5 Mouse 7.2 pKi = 7.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
CHEMBL97518 214823 0 None 1 5 Mouse 7.2 pKi = 7.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [125I]-2-iodo LSD as radioligand
ChEMBL 367 5 3 3 2.6 CC[C@@](C)(CO)CNC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1021/jm030030n
3233 10285 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3247 10285 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
6604889 10285 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
CHEMBL282199 10285 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
DB13988 10285 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
22857296 35923 0 None -123 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
CHEMBL13816 35923 0 None -123 4 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm030030n
44397433 19037 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1184710 19037 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL365084 19037 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 3 5.9 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)c1ccccc1 10.1016/j.bmcl.2005.06.024
2470 10425 50 None -77624 58 Human 4.2 pKi = 4.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
3300 10425 50 None -77624 58 Human 4.2 pKi = 4.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
5265 10425 50 None -77624 58 Human 4.2 pKi = 4.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
99 10425 50 None -77624 58 Human 4.2 pKi = 4.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
CHEMBL267930 10425 50 None -77624 58 Human 4.2 pKi = 4.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm030030n
44397429 18530 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181634 18530 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
CHEMBL186450 18530 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 491 12 1 4 5.7 COCCNCc1ccc(-c2ccc(CN(Cc3cccnc3)C(=O)/C=C/c3ccccc3)cc2)cc1 10.1016/j.bmcl.2005.06.024
44456253 19609 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1188517 19609 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536562 19609 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2cc(F)ccc2CN1 10.1016/j.bmcl.2007.10.080
3233 10285 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
3247 10285 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
6604889 10285 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
CHEMBL282199 10285 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
DB13988 10285 44 None -10 12 Human 7.2 pKi = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 5 receptorBinding affinity towards 5-hydroxytryptamine 5 receptor
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm030030n
44350898 24752 0 None -1 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1cccc3ccccc13)CC2 10.1021/jm030080s
CHEMBL126188 24752 0 None -1 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1cccc3ccccc13)CC2 10.1021/jm030080s
44350897 124851 0 None -2 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1ccc3ccccc3c1)CC2 10.1021/jm030080s
CHEMBL340511 124851 0 None -2 2 Mouse 6.2 pKi = 6.2 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 370 5 0 3 5.2 Cn1c2c(c3ccccc31)CN(CCCOc1ccc3ccccc3c1)CC2 10.1021/jm030080s
12628906 101371 28 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 147 0 2 3 0.7 NC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL25212 101371 28 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 147 0 2 3 0.7 NC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL557381 101371 28 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 147 0 2 3 0.7 NC1=Nc2ccccc2CN1 10.1016/j.bmcl.2007.10.080
135508617 136016503 17402 0 None -12 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL1170237 17402 0 None -12 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3ccc(Br)cc23)C1=O 10.1016/j.bmc.2013.09.011
145977799 170422 0 None -9 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
CHEMBL4204036 170422 0 None -9 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 257 3 1 3 2.9 C[C@@H]1SC(c2ccccc2)=N[C@@H]1Cc1c[nH]cn1 10.1021/acs.jnatprod.7b00317
44582675 196480 0 None -114 15 Human 5.2 pKi = 5.2 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A 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 -114 15 Human 5.2 pKi = 5.2 Binding
Inhibition of human cloned 5HT5A receptor by competitive binding experimentInhibition of human cloned 5HT5A 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
117209965 192026 1 None -29 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4858338 192026 1 None -29 6 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT5A receptor (unknown origin)Binding affinity to 5HT5A receptor (unknown origin)
ChEMBL 262 2 2 3 2.1 Clc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
4376990 199788 5 None -27 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 199788 5 None -27 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 199788 5 None -27 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
136118661 83032 0 None -7 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058429 83032 0 None -7 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1C 10.1016/j.bmc.2013.09.011
50923583 131935 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 356 3 2 3 2.6 COc1cccc(F)c1-c1ncc(F)c2ccc(C(=O)N=C(N)N)cc12 nan
CHEMBL3644532 131935 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.Binding Inhibition Assay: A solution of the compound to be tested and 100 μM 5-CT (5-carboxamidetriptamine) in DMSO was added to a 96-well plate at 2 μl/well, suspended in an incubation buffer, and a membrane from HEK293 cells for forced expressions of a human 5-HT5A receptor prepared at 200 ug/ml was added at 100 μl/well. After incubation at room temperature for 15 minutes, a [3H]5-CT solution (2 nM [3H]5-CT, incubation buffer) was added thereto at 100 μl/well.Separately, 100 μl of the solution was distributed into a liquid scintillation vial, and 2 ml of Aquasol II (registered trademark) was added thereto, followed by stirring. Then, radioactivity was measured by a liquid scintillation counter. It was incubated at 37C. for 60 minutes. The reaction mixture was sucked into 96-well GF/C filter plate that had been pre-treated with 0.2% polyethyleneimine, and washed six times with an ice-cooled, 50 mM Tris (pH 7.5) buffer. The GF/C filter plate was dried.
ChEMBL 356 3 2 3 2.6 COc1cccc(F)c1-c1ncc(F)c2ccc(C(=O)N=C(N)N)cc12 nan
CHEMBL5094234 222352 0 None -331 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096019 222352 0 None -331 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5091270 222080 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assayDisplacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
ChEMBL None None None O=S1(=O)CCC[C@@H](CNCc2cccc3cccnc23)C1 10.1021/acs.jmedchem.1c02031
44355201 121996 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
CHEMBL334553 121996 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 0 2 3.7 CCCN(CCC)[C@@H]1C[C@@H]1c1cccc(OC)c1 10.1016/0960-894X(96)00045-5
130442572 178687 0 None -158 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO 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 -158 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO 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
21509921 111235 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 111235 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
44351047 24854 0 None - 1 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 5 1 2 4.1 Fc1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
CHEMBL126724 24854 0 None - 1 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 5 1 2 4.1 Fc1ccc(OCCCN2CCc3[nH]c4ccccc4c3C2)cc1 10.1021/jm030080s
44351139 25616 0 None 1 3 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
CHEMBL128099 25616 0 None 1 3 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 334 6 0 3 4.5 CCn1c2c(c3ccccc31)CN(CCCOc1ccccc1)CC2 10.1021/jm030080s
21509921 111235 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 111235 0 None -74 24 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)Displacement of [3H]LSD from 5-HT5A receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
73355415 99308 0 None -38 13 Human 5.1 pKi = 5.1 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
CHEMBL2432039 99308 0 None -38 13 Human 5.1 pKi = 5.1 Binding
Inhibition of 5-HT5A receptor (unknown origin) by PDSP assayInhibition of 5-HT5A receptor (unknown origin) by PDSP assay
ChEMBL 277 3 1 1 2.1 C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42 10.1016/j.bmc.2013.07.045
44355164 29813 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
CHEMBL133020 29813 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 247 7 1 2 3.6 CCCN(CCC)C[C@H]1C[C@@H]1c1ccccc1O 10.1016/0960-894X(96)00045-5
2737389 194365 28 None -53 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
CHEMBL494675 194365 28 None -53 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysisDisplacement of [3H]LSD from human recombinant 5-HT5A receptor expressed in cell membrane after 1.5 hrs by scintillation counting analysis
ChEMBL 238 2 1 2 2.8 c1ccc(-c2ccccc2N2CCNCC2)cc1 10.1039/C8MD00313K
71459604 90568 0 None -13 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to 5-HT5A receptorBinding affinity to 5-HT5A receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 90568 0 None -13 14 Human 5.1 pKi = 5.1 Binding
Binding affinity to 5-HT5A receptorBinding affinity to 5-HT5A receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
136118620 83027 0 None -24 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL2058419 83027 0 None -24 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cccc(Br)c23)C1=O 10.1016/j.bmc.2013.09.011
44397669 18559 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181776 18559 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL191583 18559 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 531 13 1 3 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)C1CC1c1ccccc1 10.1016/j.bmcl.2005.06.024
44397362 19031 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL1184673 19031 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
CHEMBL363678 19031 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSDBinding affinity towards human 5-hydroxytryptamine receptor 5A expressed in CHO cells using the radioligand [3H]LSD
ChEMBL 527 15 1 4 6.4 CN(C)CCN(Cc1ccc(-c2ccc(CNCCOc3ccccc3)cc2)cc1)C(=O)CCC1CCCC1 10.1016/j.bmcl.2005.06.024
44455983 104371 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 189 2 2 3 2.1 CCCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
CHEMBL270840 104371 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 189 2 2 3 2.1 CCCC1NC(N)=Nc2ccccc21 10.1016/j.bmcl.2007.10.080
44456400 19606 0 None -2 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1188501 19606 0 None -2 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL2436555 19606 0 None -2 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536539 19606 0 None -2 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2ccc(Cl)cc2CN1 10.1016/j.bmcl.2007.10.080
5 6927 72 None -323 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 6927 72 None -323 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 6927 72 None -323 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 6927 72 None -323 53 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5-HT5a receptor by radioligand displacement assayBinding affinity to human 5-HT5a receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
145967795 171602 0 None -5 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
CHEMBL4218679 171602 0 None -5 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysisDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting analysis
ChEMBL 213 2 1 4 2.0 C[C@@H]1SC(c2ccsc2)=N[C@H]1CO 10.1021/acs.jnatprod.7b00317
44455973 104244 7 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 1 2 3 2.3 CCC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
CHEMBL270176 104244 7 None 1 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 209 1 2 3 2.3 CCC1NC(N)=Nc2cccc(Cl)c21 10.1016/j.bmcl.2007.10.080
160510 107904 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
CHEMBL1506260 107904 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
CHEMBL295234 107904 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity towards 5-HT5A receptorBinding affinity towards 5-HT5A receptor
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1016/j.bmcl.2003.09.027
160510 107904 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1021/acs.jmedchem.0c01887
CHEMBL1506260 107904 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1021/acs.jmedchem.0c01887
CHEMBL295234 107904 40 None -3 6 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT5AR (unknown origin) assessed as inhibition constantBinding affinity to 5-HT5AR (unknown origin) assessed as inhibition constant
ChEMBL 184 0 1 1 2.5 CC1=NCCc2c1[nH]c1ccccc21 10.1021/acs.jmedchem.0c01887
49783209 24381 0 None -14791 26 Human 5.1 pKi = 5.1 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 24381 0 None -14791 26 Human 5.1 pKi = 5.1 Binding
Binding affinity to human 5-HT5A receptorBinding affinity to human 5-HT5A receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
155551348 180736 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 5HT5A (unknown origin)Inhibition of 5HT5A (unknown origin)
ChEMBL 487 7 1 9 3.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12 10.1021/acs.jmedchem.8b01662
CHEMBL4541409 180736 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of 5HT5A (unknown origin)Inhibition of 5HT5A (unknown origin)
ChEMBL 487 7 1 9 3.7 CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12 10.1021/acs.jmedchem.8b01662
136152977 104661 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 225 2 2 3 2.2 CC1NC(NCC(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL272355 104661 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 225 2 2 3 2.2 CC1NC(NCC(F)F)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
1355 8792 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
142 8792 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
CHEMBL478 8792 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
DB12110 8792 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor was evaluated using [3H]LSD as radioligand
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
1355 8792 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
142 8792 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
CHEMBL478 8792 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
DB12110 8792 88 None -549 16 Mouse 5.1 pKi = 5.1 Binding
Binding affinity towards murine 5-hydroxytryptamine 5A receptorBinding affinity towards murine 5-hydroxytryptamine 5A receptor
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm030030n
44351103 27081 0 None -9 2 Mouse 6.1 pKi = 6.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 396 7 0 3 5.5 c1ccc(Cn2c3c(c4ccccc42)CN(CCCOc2ccccc2)CC3)cc1 10.1021/jm030080s
CHEMBL130586 27081 0 None -9 2 Mouse 6.1 pKi = 6.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 396 7 0 3 5.5 c1ccc(Cn2c3c(c4ccccc42)CN(CCCOc2ccccc2)CC3)cc1 10.1021/jm030080s
132060720 169268 0 None -2 9 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO 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 6.1 pKi = 6.1 Binding
Displacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from human 5-HT5A receptor expressed in Flp-In CHO 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
44456398 20722 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL1196644 20722 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2 10.1016/j.bmcl.2007.10.080
CHEMBL557746 20722 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 161 0 2 3 1.0 Cc1ccc2c(c1)CNC(N)=N2 10.1016/j.bmcl.2007.10.080
135464118 99835 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
CHEMBL2442272 99835 0 None -2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 304 1 4 2 1.9 N=C1NC(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1 10.1016/j.bmc.2013.09.011
44456244 104761 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2c(Cl)cccc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL272752 104761 1 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2c(Cl)cccc2CN1 10.1016/j.bmcl.2007.10.080
53325242 63844 0 None -4 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells 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 -4 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells 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
1621 9207 17 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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 -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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 -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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 -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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 -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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
10405482 25914 0 None 11 2 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 348 6 0 3 4.6 COc1ccc(CCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
CHEMBL128945 25914 0 None 11 2 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 348 6 0 3 4.6 COc1ccc(CCCCN2CCc3c(c4ccccc4n3C)C2)cc1 10.1021/jm030080s
CHEMBL5091373 222346 0 None -436 9 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 222346 0 None -436 9 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44456286 19618 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL1188596 19618 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL536790 19618 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 165 0 2 3 0.9 NC1=Nc2ccc(F)cc2CN1 10.1016/j.bmcl.2007.10.080
136118659 83030 0 None -5 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
CHEMBL2058427 83030 0 None -5 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 346 1 1 2 2.7 C/N=C1\N(C)C(=O)/C(=C\c2c[nH]c3ccc(Br)cc23)N1C 10.1016/j.bmc.2013.09.011
10881882 24964 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 4 0 3 3.8 Cn1c2c(c3ccccc31)CN(CCOc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL126994 24964 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 324 4 0 3 3.8 Cn1c2c(c3ccccc31)CN(CCOc1ccc(F)cc1)CC2 10.1021/jm030080s
122483292 144889 0 None -33 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3764335 144889 0 None -33 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
CHEMBL3765876 144889 0 None -33 7 Human 6.0 pKi = 6.0 Binding
Binding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT5 receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 1 5 5.5 O=C(CCCCCN1CCN(c2ccccc2O)CC1)n1c2ccccc2c2ccccc21 10.1016/j.ejmech.2016.01.043
44351499 125331 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(CCCCc1ccc(F)cc1)CC2 10.1021/jm030080s
CHEMBL341506 125331 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 336 5 0 2 4.7 Cn1c2c(c3ccccc31)CN(CCCCc1ccc(F)cc1)CC2 10.1021/jm030080s
130442480 182049 0 None -117 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO 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 -117 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-LSD from recombinant human 5HT5A receptor stably expressed in Flp-In CHO 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
136152967 162344 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 261 2 2 5 1.3 CC1NC(NCC2COCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
CHEMBL404365 162344 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
ChEMBL 261 2 2 5 1.3 CC1NC(NCC2COCCO2)=Nc2ccccc21 10.1016/j.bmcl.2007.10.078
135433933 183817 1 None -8 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
CHEMBL463249 183817 1 None -8 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in Flp-In CHO cells
ChEMBL 332 1 2 2 2.6 CN1C(=N)N(C)/C(=C/c2c[nH]c3cc(Br)ccc23)C1=O 10.1016/j.bmc.2013.09.011
44456207 20418 7 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL1194499 20418 7 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL552782 20418 7 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 177 1 2 4 0.7 COc1cccc2c1N=C(N)NC2 10.1016/j.bmcl.2007.10.080
CHEMBL5077293 221270 0 None -346 9 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT5AR (unknown origin)Binding affinity to 5-HT5AR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
44351184 25633 0 None 1 3 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
CHEMBL128185 25633 0 None 1 3 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligandBinding affinity towards mouse 5-hydroxytryptamine 5A receptor using LSD as radioligand
ChEMBL 368 6 0 4 4.2 COc1ccc2c(c1)c1c(n2C)CCN(CCCOc2ccc(F)cc2)C1 10.1021/jm030080s
23642275 7270 31 None -60 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysis
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
8433 7270 31 None -60 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysis
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
CHEMBL2164327 7270 31 None -60 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysisDisplacement of [3H]LSD from recombinant human 5-HT5a receptor after 120 mins by scintillation counting analysis
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.1039/C8MD00313K
13702393 161804 2 None 6 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL401541 161804 2 None 6 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
CHEMBL556983 161804 2 None 6 6 Human 7.0 pKi = 7 Binding
Displacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cellsDisplacement of [3H]LSD from human recombinant 5HT5A receptor expressed in HEK293-EBNA cells
ChEMBL 181 0 2 3 1.4 NC1=Nc2cccc(Cl)c2CN1 10.1016/j.bmcl.2007.10.080
118464427 145112 0 None -36 7 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3771331 145112 0 None -36 7 Human 6.0 pKi = 6 Binding
Displacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]LSD from 5-HT5A receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 328 3 4 6 1.8 CCNC(=O)c1cccc(NC2=NC(N)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
44355200 33110 0 None - 1 Rat 6.0 pKi = 6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
CHEMBL135894 33110 0 None - 1 Rat 6.0 pKi = 6 Binding
Inhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranesInhibition of specific [3H]OH-DPAT binding at 5-hydroxytryptamine 1A receptor in rat hippocampal membranes
ChEMBL 261 8 0 2 3.9 CCCN(CCC)C[C@@H]1C[C@@H]1c1ccccc1OC 10.1016/0960-894X(96)00045-5
2543 10479 68 None -1412 32 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 None -1412 32 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 None -1412 32 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 None -1412 32 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 None -1412 32 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortexDisplacement of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor from pig cortex
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
4106 9280 22 3H-5CT -14 33 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-5CT -14 33 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-5CT -14 33 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-5CT -14 33 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 9280 22 125I-LSD -269 33 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 125I-LSD -269 33 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 125I-LSD -269 33 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 125I-LSD -269 33 Mouse 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1220 6975 55 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 125I-LSD -794 44 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
10257 7525 31 125I-LSD -741 19 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 7525 31 125I-LSD -741 19 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 7525 31 125I-LSD -741 19 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 7525 31 125I-LSD -741 19 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
135398737 7745 93 3H-5CT -173 90 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-5CT -173 90 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-5CT -173 90 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-5CT -173 90 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-5CT -173 90 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11957541 8241 40 125I-LSD -229 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 8241 40 125I-LSD -229 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 8241 40 125I-LSD -229 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 8241 40 125I-LSD -229 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 8241 40 125I-LSD -229 16 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
681 8247 72 125I-LSD -199 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 125I-LSD -199 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 125I-LSD -199 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 125I-LSD -199 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 125I-LSD -199 38 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1357 9263 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
1672 9263 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
224 9263 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
896 9263 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
CHEMBL45 9263 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
DB01065 9263 139 125I-LSD -3311 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 232 4 2 2 1.9 COc1ccc2c(c1)c(CCNC(=O)C)c[nH]2 None
206 9271 16 125I-LSD -676 25 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 9271 16 125I-LSD -676 25 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 9271 16 125I-LSD -676 25 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
133 9274 52 125I-LSD -1862 43 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 125I-LSD -1862 43 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 125I-LSD -1862 43 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 125I-LSD -1862 43 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 125I-LSD -1862 43 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
134 9292 24 125I-LSD -109 67 Rat 6.0 pKi = 6 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 125I-LSD -109 67 Rat 6.0 pKi = 6 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 125I-LSD -109 67 Rat 6.0 pKi = 6 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 125I-LSD -109 67 Rat 6.0 pKi = 6 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 125I-LSD -109 67 Rat 6.0 pKi = 6 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
484 9633 51 125I-LSD -31 35 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 125I-LSD -31 35 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 125I-LSD -31 35 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
1243 10390 34 125I-LSD -3235 5 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
944 10390 34 125I-LSD -3235 5 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
CHEMBL324017 10390 34 125I-LSD -3235 5 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
102 10899 48 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
102 10899 48 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 125I-LSD -1698 49 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 125I-LSD -2511 49 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
108182 10903 22 125I-LSD -3 17 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 125I-LSD -3 17 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 125I-LSD -3 17 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
None 223158 0 UNDEFINED -1122 11 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
179 7188 115 3H-LSD -4365 50 Human 5.0 pKi = 5 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-LSD -4365 50 Human 5.0 pKi = 5 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-LSD -4365 50 Human 5.0 pKi = 5 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-LSD -4365 50 Human 5.0 pKi = 5 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-LSD -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
681 8247 72 125I-LSD -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 125I-LSD -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 125I-LSD -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 125I-LSD -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 125I-LSD -1995 38 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1524 8962 96 125I-LSD -7585 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 125I-LSD -7585 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 125I-LSD -7585 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 125I-LSD -7585 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 125I-LSD -7585 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 125I-LSD -7585 51 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
134 9292 24 3H-LSD -162 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-LSD -162 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-LSD -162 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-LSD -162 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-LSD -162 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
484 9633 51 125I-LSD -100 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
484 9633 51 3H-KETANSERIN -31 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 125I-LSD -100 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 3H-KETANSERIN -31 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 125I-LSD -100 35 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 3H-KETANSERIN -31 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
15897 9637 0 3H-LSD -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-LSD -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-LSD -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
119570 9933 96 3H-LSD -4570 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 3H-LSD -4570 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 3H-LSD -4570 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 3H-LSD -4570 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 3H-LSD -4570 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
243 9976 91 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 9976 91 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 9976 91 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 9976 91 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 9976 91 3H-5CT -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
173 10036 95 3H-LSD -114 23 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 3H-LSD -114 23 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 3H-LSD -114 23 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
2402 10143 62 3H-LSD -549 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 10143 62 3H-LSD -549 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 10143 62 3H-LSD -549 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 10143 62 3H-LSD -549 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 10143 62 3H-LSD -549 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
128563 10237 33 3H-LSD -2398 42 Human 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-LSD -2398 42 Human 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-LSD -2398 42 Human 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-LSD -2398 42 Human 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
2543 10479 68 125I-LSD -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 10479 68 UNDEFINED -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 125I-LSD -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 UNDEFINED -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 125I-LSD -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 UNDEFINED -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 125I-LSD -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 UNDEFINED -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 125I-LSD -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 UNDEFINED -257 32 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
185 10778 60 3H-LSD -30902 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-LSD -30902 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-LSD -30902 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-LSD -30902 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
102 10899 48 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-LSD -1698 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2662 18156 131 3H-Alpha-Me-histamine -41 30 Guinea pig 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-Alpha-Me-histamine -41 30 Guinea pig 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
5090 22333 106 3H-Alpha-Me-histamine -1348 30 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 22333 106 3H-Alpha-Me-histamine -1348 30 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
10297 33885 30 3H-LSD -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-LSD -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-LSD -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-LSD -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-LSD -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
21830793 98610 10 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 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 -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
2244 101008 100 3H-LSD -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-LSD -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
3663 106743 83 3H-LSD -288 28 Human 5.0 pKi = 5 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-LSD -288 28 Human 5.0 pKi = 5 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
446220 140299 14 3H-LSD -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-LSD -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-LSD -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-LSD -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
5280343 195054 124 3H-LSD -147 31 Human 5.0 pKi = 5 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-LSD -147 31 Human 5.0 pKi = 5 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-LSD -147 31 Human 5.0 pKi = 5 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
54676228 200394 112 3H-LSD -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-LSD -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-LSD -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-LSD -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-LSD -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-LSD -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-LSD -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-LSD -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-LSD -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-LSD -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-LSD -275 32 Human 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-LSD -275 32 Human 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
1973 210262 15 3H-LSD -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 210262 15 3H-LSD -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 210262 15 3H-LSD -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
202478 211466 20 3H-LSD -52 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 211466 20 3H-LSD -52 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
3821 211497 17 3H-LSD -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-LSD -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
5311189 211620 11 3H-LSD -112 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 211620 11 3H-LSD -112 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 212120 21 3H-LSD -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 212120 21 3H-LSD -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 212120 21 3H-LSD -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
119607 212982 113 3H-Alpha-Me-histamine -97 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
CHEMBL865 212982 113 3H-Alpha-Me-histamine -97 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
3337 213146 27 3H-LSD -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-LSD -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-LSD -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-LSD -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-LSD -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
165193 222724 0 125I-LSD -42657 30 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 125I-LSD -42657 30 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 125I-LSD -42657 30 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
None 222772 0 3H-LSD -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-LSD -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-LSD -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-LSD -95499 29 Human 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-LSD -1 34 Human 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-LSD -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 223092 0 3H-LSD -1 34 Human 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-LSD -1 34 Human 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-LSD -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 223095 0 3H-LSD -1 40 Human 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-LSD -1 39 Human 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-LSD -1 30 Human 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-LSD -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-LSD -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-LSD -16 27 Human 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
4978 223107 0 3H-LSD -7 27 Human 5.0 pKi = 5 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
None 223108 0 3H-LSD -3 27 Human 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-LSD -281 27 Human 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-LSD -1 27 Human 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-LSD -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-LSD -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-LSD -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-LSD -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
123619 223172 0 3H-Alpha-Me-histamine -1412 27 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 223173 0 3H-Alpha-Me-histamine -1 29 Guinea pig 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 223174 0 3H-Alpha-Me-histamine -7 28 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
5 6927 72 3H-LSD -891 53 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-LSD -891 53 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-LSD -891 53 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-LSD -891 53 Mouse 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
2726 7706 68 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-LSD -16 72 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1809 6922 32 UNDEFINED -257 37 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 6922 32 125I-LSD -363 37 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 UNDEFINED -257 37 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 125I-LSD -363 37 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 UNDEFINED -257 37 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 125I-LSD -363 37 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
135398745 9688 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
242 7258 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 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-LSD -144 51 Human 5.9 pKi = 5.9 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-LSD -144 51 Human 5.9 pKi = 5.9 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-LSD -144 51 Human 5.9 pKi = 5.9 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-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 7258 124 3H-LSD -144 51 Human 5.9 pKi = 5.9 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-LSD -144 51 Human 5.9 pKi = 5.9 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-LSD -144 51 Human 5.9 pKi = 5.9 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-LSD -144 51 Human 5.9 pKi = 5.9 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-LSD -144 51 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
4106 9280 22 UNDEFINED -269 33 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 UNDEFINED -269 33 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 UNDEFINED -269 33 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 UNDEFINED -269 33 Mouse 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1220 6975 55 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 125I-LSD -1071 44 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
5 6927 72 3H-5CT -323 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5CT -323 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5CT -323 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5CT -323 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 125I-LSD -999 53 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 125I-LSD -999 53 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 125I-LSD -999 53 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 125I-LSD -999 53 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
103 10925 61 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-LSD -25 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
7153 104796 77 3H-LSD -70 33 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 3H-LSD -70 33 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
135398745 9688 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-LSD -109 65 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11954224 222732 0 3H-LSD -147 59 Human 7.9 pKi = 7.9 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
1212 8443 50 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-LSD -63 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
4106 9280 22 125I-LSD -128 33 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 125I-LSD -128 33 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 125I-LSD -128 33 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 125I-LSD -128 33 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
11954224 222732 0 125I-LSD -131 59 Rat 7.8 pKi = 7.8 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
1809 6922 32 125I-LSD -257 37 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 125I-LSD -257 37 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 125I-LSD -257 37 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4452 9538 19 3H-LSD -52480 18 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 9538 19 3H-LSD -52480 18 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 9538 19 3H-LSD -52480 18 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
1220 6975 55 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 UNDEFINED -1071 44 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
None 222914 0 3H-LSD -1819 23 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
134 9292 24 125I-LSD -109 67 Rat 6.7 pKi = 6.7 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 125I-LSD -109 67 Rat 6.7 pKi = 6.7 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 125I-LSD -109 67 Rat 6.7 pKi = 6.7 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 125I-LSD -109 67 Rat 6.7 pKi = 6.7 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 125I-LSD -109 67 Rat 6.7 pKi = 6.7 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
2389 10104 118 3H-LSD -346 66 Human 6.7 pKi = 6.7 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-LSD -346 66 Human 6.7 pKi = 6.7 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-LSD -346 66 Human 6.7 pKi = 6.7 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-LSD -346 66 Human 6.7 pKi = 6.7 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-LSD -346 66 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1809 6922 32 3H-5CT -229 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5CT -229 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5CT -229 37 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
6971132 222788 0 3H-LSD -512 14 Mouse 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
1524 8962 96 3H-5CT -1862 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-5CT -1862 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-5CT -1862 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-5CT -1862 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-5CT -1862 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-5CT -1862 51 Human 4.7 pKi = 4.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2389 10104 118 3H-LSD -346 66 Human 6.7 pKi = 6.7 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-LSD -346 66 Human 6.7 pKi = 6.7 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-LSD -346 66 Human 6.7 pKi = 6.7 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-LSD -346 66 Human 6.7 pKi = 6.7 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-LSD -346 66 Human 6.7 pKi = 6.7 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-LSD -77 85 Human 5.7 pKi = 5.7 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-LSD -77 85 Human 5.7 pKi = 5.7 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-LSD -77 85 Human 5.7 pKi = 5.7 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-LSD -77 85 Human 5.7 pKi = 5.7 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-LSD -77 85 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
242 7258 124 3H-LSD -144 51 Human 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-LSD -144 51 Human 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-LSD -144 51 Human 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-LSD -144 51 Human 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-LSD -144 51 Human 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
2337 10030 77 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-LSD -38 62 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1809 6922 32 125I-LSD -363 37 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 125I-LSD -363 37 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 125I-LSD -363 37 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
5 6927 72 125I-LSD -999 53 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 125I-LSD -999 53 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 125I-LSD -999 53 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 125I-LSD -999 53 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1220 6975 55 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-5CT -1548 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
5 6927 72 125I-LSD -891 53 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 UNDEFINED -891 53 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 125I-LSD -891 53 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 UNDEFINED -891 53 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 125I-LSD -891 53 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 UNDEFINED -891 53 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 125I-LSD -891 53 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 UNDEFINED -891 53 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
115 10563 80 125I-LSD -61 27 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 125I-LSD -61 27 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 125I-LSD -61 27 Mouse 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
145 6928 49 3H-LSD -53 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 6928 49 3H-LSD -53 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 6928 49 3H-LSD -53 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 6928 49 3H-LSD -53 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115237 62359 119 3H-LSD -181 54 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-LSD -181 54 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
4106 9280 22 125I-LSD -128 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 125I-LSD -128 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 125I-LSD -128 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 125I-LSD -128 33 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
103 10925 61 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-LSD -25 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
10257 7525 31 3H-LSD -741 19 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 7525 31 3H-LSD -741 19 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 7525 31 3H-LSD -741 19 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 7525 31 3H-LSD -741 19 Mouse 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
2865 10915 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 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-LSD -169 53 Human 6.5 pKi = 6.5 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-LSD -169 53 Human 6.5 pKi = 6.5 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-LSD -169 53 Human 6.5 pKi = 6.5 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-LSD -169 53 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1588 9105 27 3H-LSD -8 44 Human 8.5 pKi = 8.5 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-LSD -8 44 Human 8.5 pKi = 8.5 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-LSD -8 44 Human 8.5 pKi = 8.5 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-LSD -8 44 Human 8.5 pKi = 8.5 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-LSD -8 44 Human 8.5 pKi = 8.5 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
11954224 222732 0 125I-LSD -131 59 Mouse 8.4 pKi = 8.4 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
2865 10915 73 3H-LSD -169 53 Human 6.5 pKi = 6.5 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-LSD -169 53 Human 6.5 pKi = 6.5 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-LSD -169 53 Human 6.5 pKi = 6.5 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-LSD -169 53 Human 6.5 pKi = 6.5 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-LSD -169 53 Human 6.5 pKi = 6.5 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-LSD -38 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-LSD -38 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-LSD -38 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-LSD -38 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-LSD -38 62 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
None 222725 0 125I-LSD -223 24 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 223057 0 3H-LSD -3630 12 Human 6.5 pKi = 6.5 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
11954259 222758 0 3H-LSD -1202 43 Human 6.4 pKi = 6.4 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
100 10577 58 3H-LSD -23 54 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-LSD -23 54 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-LSD -23 54 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-LSD -23 54 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-LSD -23 54 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
11954224 222732 0 3H-LSD -131 59 Mouse 7.4 pKi = 7.4 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
135398737 7745 93 3H-LSD -173 90 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-LSD -173 90 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-LSD -173 90 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-LSD -173 90 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-LSD -173 90 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
3294 8787 111 3H-LSD -676 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-LSD -676 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-LSD -676 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-LSD -676 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-LSD -676 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2470 10425 50 None -77624 58 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 None -77624 58 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 None -77624 58 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 None -77624 58 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 None -77624 58 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1524 8962 96 None -1862 51 Human 8.3 pKi = 8.3 Binding
NoneNone
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 -1862 51 Human 8.3 pKi = 8.3 Binding
NoneNone
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 -1862 51 Human 8.3 pKi = 8.3 Binding
NoneNone
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 -1862 51 Human 8.3 pKi = 8.3 Binding
NoneNone
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 -1862 51 Human 8.3 pKi = 8.3 Binding
NoneNone
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 -1862 51 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
2543 10479 68 None -257 32 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 None -257 32 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 None -257 32 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 None -257 32 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 None -257 32 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1342 6824 49 3H-LSD -16 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 6824 49 3H-LSD -16 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 6824 49 3H-LSD -16 19 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
135398737 7745 93 None -67 90 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -67 90 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -67 90 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -67 90 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -67 90 Mouse 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
102 10899 48 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 None -407 49 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
216239 30567 118 None -6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1200485 30567 118 None -6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
CHEMBL1336 30567 118 None -6 7 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counterDisplacement of [3H]LSD from 5HT5A receptor after 1.5 hrs by scintillation counter
Drug Central 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 None
2337 10030 77 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 None -38 62 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1353 8692 93 None -77 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 None -77 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 None -77 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 None -77 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 None -77 85 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
242 7258 124 None -144 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 -144 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 -144 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 -144 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 -144 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
134 9292 24 3H-LSD -67 67 Mouse 6.3 pKi = 6.3 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-LSD -67 67 Mouse 6.3 pKi = 6.3 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-LSD -67 67 Mouse 6.3 pKi = 6.3 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-LSD -67 67 Mouse 6.3 pKi = 6.3 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-LSD -67 67 Mouse 6.3 pKi = 6.3 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
2543 10479 68 3H-5CT -1412 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5CT -1412 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5CT -1412 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5CT -1412 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5CT -1412 32 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2435 10362 83 3H-LSD -999 48 Human 6.3 pKi = 6.3 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-LSD -999 48 Human 6.3 pKi = 6.3 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-LSD -999 48 Human 6.3 pKi = 6.3 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-LSD -999 48 Human 6.3 pKi = 6.3 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-LSD -999 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1809 6922 32 3H-LSD -257 37 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-LSD -257 37 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-LSD -257 37 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
3294 8787 111 3H-LSD -676 44 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-LSD -676 44 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-LSD -676 44 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-LSD -676 44 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-LSD -676 44 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
277 8083 62 3H-LSD -69 50 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 3H-LSD -69 50 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 3H-LSD -69 50 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 3H-LSD -69 50 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 3H-LSD -69 50 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
135398737 7745 93 None -173 90 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -173 90 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -173 90 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -173 90 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -173 90 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligandBinding affinity towards human 5-hydroxytryptamine 5A receptor was evaluated using [3H]-5-CT as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
33630 185736 99 None -13 28 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells 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]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells by radioligand binding assayDisplacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In CHO cells 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
102 10899 48 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 None -1698 49 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
5022 8432 76 None -1 9 Human 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 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 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 None
1613 9127 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 None -19 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
133 9274 52 None -251 43 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 None -251 43 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 None -251 43 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 None -251 43 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 None -251 43 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
11954224 222732 0 UNDEFINED -131 59 Mouse 8.2 pKi = 8.2 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
11954224 222732 0 125I-LSD -131 59 Rat 8.2 pKi = 8.2 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
100 10577 58 None -23 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 None -23 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 None -23 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 None -23 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 None -23 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 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
2865 10915 73 None -169 53 Human 8.2 pKi = 8.2 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 -169 53 Human 8.2 pKi = 8.2 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 -169 53 Human 8.2 pKi = 8.2 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 -169 53 Human 8.2 pKi = 8.2 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 -169 53 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
115237 62359 119 None -181 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 None -181 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
4806 10780 88 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 10780 88 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 10780 88 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 10780 88 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 10780 88 None -10 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to human 5HT5A receptorBinding affinity to human 5HT5A receptor
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
2389 10104 118 None -346 66 Human 8.2 pKi = 8.2 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 -346 66 Human 8.2 pKi = 8.2 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 -346 66 Human 8.2 pKi = 8.2 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 -346 66 Human 8.2 pKi = 8.2 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 -346 66 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
134 9292 24 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None -109 67 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1212 8443 50 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 None -63 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3389 224490 0 None -1 26 Human 8.2 pKi = 8.2 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
11978813 7508 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 7508 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 7508 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 7508 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 7508 79 None -8 24 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
22530 62904 58 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
CHEMBL1600878 62904 58 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
CHEMBL1625607 62904 58 None -1 3 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 None
2726 7706 68 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 None -16 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
141 8209 35 3H-LSD -7 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 8209 35 3H-LSD -7 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 8209 35 3H-LSD -7 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 8209 35 3H-LSD -7 22 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
134 9292 24 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 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 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 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 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 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 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 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 I125-2-iodo LSD -67 67 Mouse 7.2 pKi = 7.2 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
134 9292 24 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 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 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 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 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 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 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 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 125I-LSD -67 67 Mouse 7.2 pKi = 7.2 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
133 9274 52 3H-5CT -251 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 3H-5CT -251 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 3H-5CT -251 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 3H-5CT -251 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 3H-5CT -251 43 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
102 10899 48 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 UNDEFINED -1698 49 Mouse 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2470 10425 50 3H-5CT -77624 58 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-5CT -77624 58 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-5CT -77624 58 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-5CT -77624 58 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-5CT -77624 58 Human 4.2 pKi = 4.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
107780 8625 54 3H-5HT -6760 18 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 3H-5HT -6760 18 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 3H-5HT -6760 18 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
134 9292 24 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 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 None -162 67 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 9292 24 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 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 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 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 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 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 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 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 None -67 67 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
103 10925 61 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 None -25 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
11954224 222732 0 None -147 59 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation countingDisplacement of [3H]LSD from 5-HT5A receptor after 1.5 hrs by scintillation counting
Drug Central 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
1613 9127 53 3H-LSD -19 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-LSD -19 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-LSD -19 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-LSD -19 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-LSD -19 44 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
134 9292 24 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 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 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 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 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 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 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 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 UNDEFINED -67 67 Mouse 7.1 pKi = 7.1 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
1621 9207 17 None -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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 -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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 -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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 -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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 -27 44 Human 8.1 pKi = 8.1 Binding
Binding affinities towards 5-hydroxytryptamine 5A receptorBinding affinities towards 5-hydroxytryptamine 5A receptor
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
11954224 222732 0 None -131 59 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 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
11954224 222732 0 None -131 59 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 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
46780481 114308 20 None -50 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 -50 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 -50 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 -50 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1621 9207 17 3H-LSD -28 44 Rat 8.1 pKi = 8.1 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-LSD -28 44 Rat 8.1 pKi = 8.1 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-LSD -28 44 Rat 8.1 pKi = 8.1 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-LSD -28 44 Rat 8.1 pKi = 8.1 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-LSD -28 44 Rat 8.1 pKi = 8.1 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
6971132 222788 0 3H-LSD -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
4806 10780 88 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
7351 10780 88 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
9966051 10780 88 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
CHEMBL2104993 10780 88 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
DB09068 10780 88 None -10 13 Human 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
11168182 10307 25 None 50 13 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 16002289
264 10307 25 None 50 13 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 16002289
CHEMBL1181770 10307 25 None 50 13 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 16002289
135398745 9688 112 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 None -109 65 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1524 8962 96 None -1862 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
197 8962 96 None -1862 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
3822 8962 96 None -1862 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
88 8962 96 None -1862 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
CHEMBL51 8962 96 None -1862 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
DB12465 8962 96 None -1862 51 Human 4.7 pKi None 4.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 7988681
2543 10479 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
2543 10479 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
5358 10479 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
5358 10479 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
54 10479 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
54 10479 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
CHEMBL128 10479 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
CHEMBL128 10479 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
DB00669 10479 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
DB00669 10479 68 None -257 32 Mouse 4.8 pKi None 4.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8450829
2303 9961 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
4946 9961 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
564 9961 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
63 9961 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
91536 9961 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
CHEMBL27 9961 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
CHEMBL452861 9961 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
DB00571 9961 68 None -17378 26 Human 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 7988681
135398737 7745 93 None -67 90 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
38 7745 93 None -67 90 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
722 7745 93 None -67 90 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
CHEMBL42 7745 93 None -67 90 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
DB00363 7745 93 None -67 90 Mouse 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
12 8335 17 None -208 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
6918513 8335 17 None -208 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
CHEMBL267615 8335 17 None -208 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 246 5 1 2 2.8 CCc1[nH]c2c(c1CCN(C)C)cc(cc2)OC 10715164
6918515 9390 38 None -158 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
71 9390 38 None -158 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
CHEMBL7318 9390 38 None -158 7 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 294 5 1 2 3.9 COc1ccc2c(c1)c(CCN(C)C)c([nH]2)c1ccccc1 10715164
2543 10479 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
2543 10479 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
5358 10479 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
5358 10479 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
54 10479 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
54 10479 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
CHEMBL128 10479 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
CHEMBL128 10479 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
DB00669 10479 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11343685
DB00669 10479 68 None -1412 32 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 7988681
102 10899 48 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
3659 10899 48 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
8969 10899 48 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
CHEMBL15245 10899 48 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
DB01392 10899 48 None -407 49 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 7988681
102 10899 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
102 10899 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
3659 10899 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
3659 10899 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
8969 10899 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
8969 10899 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
CHEMBL15245 10899 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
CHEMBL15245 10899 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
DB01392 10899 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8450829
DB01392 10899 48 None -1698 49 Mouse 5.5 pKi None 5.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8549774
115 10563 80 None -61 27 Mouse 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450829
4296 10563 80 None -61 27 Mouse 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450829
CHEMBL274866 10563 80 None -61 27 Mouse 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8450829
10257 7525 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
10257 7525 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
144 7525 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
144 7525 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
CHEMBL416526 7525 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
CHEMBL416526 7525 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
DB01445 7525 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8450829
DB01445 7525 31 None -741 19 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 8549774
1220 6975 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
1220 6975 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
31 6975 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
31 6975 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
7 6975 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
7 6975 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
CHEMBL56 6975 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
CHEMBL56 6975 55 None -1548 44 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 7988681
122130461 9206 0 None -1584 2 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 268 1 2 2 2.1 CN1C[C@@H](C=C2C1Cc1c[nH]c3c1c2ccc3)C(=O)O 8549774
139 9206 0 None -1584 2 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 268 1 2 2 2.1 CN1C[C@@H](C=C2C1Cc1c[nH]c3c1c2ccc3)C(=O)O 8549774
6717 9206 0 None -1584 2 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 268 1 2 2 2.1 CN1C[C@@H](C=C2C1Cc1c[nH]c3c1c2ccc3)C(=O)O 8549774
1220 6975 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
1220 6975 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
31 6975 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
31 6975 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
7 6975 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
7 6975 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
CHEMBL56 6975 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 11343685
CHEMBL56 6975 55 None -1071 44 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 8450829
108029 10187 57 None -1000 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 7988681
23 10187 57 None -1000 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 7988681
CHEMBL18785 10187 57 None -1000 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 7988681
197706 8246 0 None -3981 10 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
39 8246 0 None -3981 10 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
CHEMBL1742428 8246 0 None -3981 10 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
133 9274 52 None -251 43 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
1723 9274 52 None -251 43 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
28693 9274 52 None -251 43 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
CHEMBL19215 9274 52 None -251 43 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
DB13520 9274 52 None -251 43 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 7988681
135398737 7745 93 None -173 90 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
135398737 7745 93 None -173 90 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
38 7745 93 None -173 90 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
38 7745 93 None -173 90 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
722 7745 93 None -173 90 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
722 7745 93 None -173 90 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
CHEMBL42 7745 93 None -173 90 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
CHEMBL42 7745 93 None -173 90 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
DB00363 7745 93 None -173 90 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 11343685
DB00363 7745 93 None -173 90 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 7988681
5 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
5 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
5202 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5202 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
5202 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
CHEMBL39 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
CHEMBL39 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
CHEMBL39 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
DB08839 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
DB08839 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8450829
DB08839 6927 72 None -891 53 Mouse 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8549774
108029 10187 57 None -316 13 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450829
23 10187 57 None -316 13 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450829
CHEMBL18785 10187 57 None -316 13 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 8450829
5 6927 72 None -999 53 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
5202 6927 72 None -999 53 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
CHEMBL39 6927 72 None -999 53 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
DB08839 6927 72 None -999 53 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7682702
134 9292 24 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
1775 9292 24 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
9681 9292 24 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
CHEMBL1065 9292 24 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
DB00247 9292 24 None -109 67 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7682702
134 9292 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
134 9292 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
1775 9292 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
1775 9292 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
9681 9292 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
9681 9292 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
CHEMBL1065 9292 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
CHEMBL1065 9292 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
DB00247 9292 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8450829
DB00247 9292 24 None -67 67 Mouse 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8549774
5 6927 72 None -323 53 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5 6927 72 None -323 53 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
5202 6927 72 None -323 53 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
5202 6927 72 None -323 53 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
CHEMBL39 6927 72 None -323 53 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
CHEMBL39 6927 72 None -323 53 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
DB08839 6927 72 None -323 53 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11343685
DB08839 6927 72 None -323 53 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 7988681
4106 9280 22 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
4106 9280 22 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
5358812 9280 22 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
5358812 9280 22 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
89 9280 22 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
89 9280 22 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
CHEMBL93240 9280 22 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
CHEMBL93240 9280 22 None -269 33 Mouse 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8450829
134 9292 24 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
1775 9292 24 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
9681 9292 24 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
CHEMBL1065 9292 24 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
DB00247 9292 24 None -162 67 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 7988681
5074 10105 80 None -69 30 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
97 10105 80 None -69 30 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
CHEMBL267777 10105 80 None -69 30 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
DB12693 10105 80 None -69 30 Mouse 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
4106 9280 22 None -128 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
5358812 9280 22 None -128 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
89 9280 22 None -128 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
CHEMBL93240 9280 22 None -128 33 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7682702
1809 6922 32 None -257 37 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
1809 6922 32 None -257 37 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450829
1809 6922 32 None -257 37 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8549774
4 6922 32 None -257 37 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
4 6922 32 None -257 37 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450829
4 6922 32 None -257 37 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8549774
CHEMBL18840 6922 32 None -257 37 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
CHEMBL18840 6922 32 None -257 37 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8450829
CHEMBL18840 6922 32 None -257 37 Mouse 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8549774
5074 10105 80 None -43 30 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
97 10105 80 None -43 30 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
CHEMBL267777 10105 80 None -43 30 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
DB12693 10105 80 None -43 30 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 11343685
1809 6922 32 None -229 37 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
1809 6922 32 None -229 37 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7988681
4 6922 32 None -229 37 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
4 6922 32 None -229 37 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7988681
CHEMBL18840 6922 32 None -229 37 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 11343685
CHEMBL18840 6922 32 None -229 37 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7988681
1043 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
1043 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8450829
1043 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8549774
149 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
149 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8450829
149 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8549774
8223 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
8223 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8450829
8223 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8549774
CHEMBL442 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
CHEMBL442 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8450829
CHEMBL442 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8549774
DB00696 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
DB00696 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8450829
DB00696 8363 14 None -138 29 Mouse 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8549774
1809 6922 32 None -363 37 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7682702
4 6922 32 None -363 37 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7682702
CHEMBL18840 6922 32 None -363 37 Rat 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 7682702
1043 8363 14 None -69 29 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7682702
149 8363 14 None -69 29 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7682702
8223 8363 14 None -69 29 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7682702
CHEMBL442 8363 14 None -69 29 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7682702
DB00696 8363 14 None -69 29 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7682702
1043 8363 14 None -169 29 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
1043 8363 14 None -169 29 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7988681
149 8363 14 None -169 29 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
149 8363 14 None -169 29 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7988681
8223 8363 14 None -169 29 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
8223 8363 14 None -169 29 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7988681
CHEMBL442 8363 14 None -169 29 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
CHEMBL442 8363 14 None -169 29 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7988681
DB00696 8363 14 None -169 29 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 11343685
DB00696 8363 14 None -169 29 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 7988681
4106 9280 22 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
4106 9280 22 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681
5358812 9280 22 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
5358812 9280 22 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681
89 9280 22 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
89 9280 22 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681
CHEMBL93240 9280 22 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11343685
CHEMBL93240 9280 22 None -14 33 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 7988681