Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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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
5803 7182 21 None -2 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1016/j.bmc.2018.09.015
854189 7182 21 None -2 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1016/j.bmc.2018.09.015
CHEMBL594671 7182 21 None -2 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1016/j.bmc.2018.09.015
46235794 169714 0 None 2 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 414 7 1 4 4.8 CN(C(=O)[C@@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4174307 169714 0 None 2 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 414 7 1 4 4.8 CN(C(=O)[C@@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
67209751 168948 0 None -3 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 505 10 1 6 6.0 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC3CCCC3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
CHEMBL4162307 168948 0 None -3 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 505 10 1 6 6.0 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC3CCCC3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
117898644 169876 0 None -3 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 515 10 1 7 5.7 CC(C)C[C@H](CC(=O)O)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4177037 169876 0 None -3 2 Mouse 7.0 pEC50 = 7 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 515 10 1 7 5.7 CC(C)C[C@H](CC(=O)O)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
145953626 169290 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 423 4 1 3 5.3 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4167577 169290 0 None - 1 Human 5.0 pEC50 = 5 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 423 4 1 3 5.3 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
145953603 169259 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 432 4 1 5 4.3 C#Cc1ccccc1[C@H]1SC[C@@H](C(=O)O)N1C(=O)c1ccc(-c2c(C)noc2C)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4167161 169259 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 432 4 1 5 4.3 C#Cc1ccccc1[C@H]1SC[C@@H](C(=O)O)N1C(=O)c1ccc(-c2c(C)noc2C)cc1 10.1021/acs.jmedchem.8b00855
145953670 169341 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 424 4 1 4 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4168456 169341 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 424 4 1 4 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
162666399 189164 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assayAgonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assay
ChEMBL 468 6 2 4 3.8 CC(Oc1cccc(Cl)c1)C(=O)N(C)[C@H]1CC[C@]2(CC1)NC(=N)N(Cc1ccccc1)C2=O 10.1016/j.bmcl.2020.127460
CHEMBL4785193 189164 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assayAgonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assay
ChEMBL 468 6 2 4 3.8 CC(Oc1cccc(Cl)c1)C(=O)N(C)[C@H]1CC[C@]2(CC1)NC(=N)N(Cc1ccccc1)C2=O 10.1016/j.bmcl.2020.127460
57520598 8593 33 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00855
8417 8593 33 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00855
CHEMBL3353541 8593 33 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00855
DB15406 8593 33 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/acs.jmedchem.8b00855
145951537 169488 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 537 10 1 7 6.0 COc1ccc(-c2ccc(Cl)cc2-c2csc(N(C(=O)[C@@H](CC(=O)O)Cc3ccco3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
CHEMBL4170829 169488 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 537 10 1 7 6.0 COc1ccc(-c2ccc(Cl)cc2-c2csc(N(C(=O)[C@@H](CC(=O)O)Cc3ccco3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
53302677 169626 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 474 8 1 4 5.9 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4172928 169626 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 474 8 1 4 5.9 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
67258265 169507 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 435 5 1 3 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4171128 169507 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 435 5 1 3 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145957026 168987 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4162808 168987 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.8b00855
117898634 169174 0 None -5 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 479 10 1 6 5.5 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC(C)C)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
CHEMBL4165748 169174 0 None -5 2 Mouse 6.9 pEC50 = 6.9 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 479 10 1 6 5.5 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC(C)C)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
145971768 169900 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 448 4 1 4 5.2 N#Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4177359 169900 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 448 4 1 4 5.2 N#Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
145971768 169900 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 448 4 1 4 5.2 N#Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4177359 169900 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 448 4 1 4 5.2 N#Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
145954653 169417 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 420 5 1 5 4.1 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccn2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4169673 169417 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 420 5 1 5 4.1 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccn2)cc1 10.1021/acs.jmedchem.8b00855
53302677 169626 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assayAgonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assay
ChEMBL 474 8 1 4 5.9 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 10.1016/j.bmcl.2020.127460
CHEMBL4172928 169626 1 None 1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assayAgonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assay
ChEMBL 474 8 1 4 5.9 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 10.1016/j.bmcl.2020.127460
145951076 169752 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 408 4 1 5 4.3 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4175033 169752 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 408 4 1 5 4.3 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
145954653 169417 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 420 5 1 5 4.1 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccn2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4169673 169417 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 420 5 1 5 4.1 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccn2)cc1 10.1021/acs.jmedchem.8b00855
145953670 169341 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 424 4 1 4 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4168456 169341 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 424 4 1 4 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
5803 7182 21 None 2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1016/j.bmc.2018.09.015
854189 7182 21 None 2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1016/j.bmc.2018.09.015
CHEMBL594671 7182 21 None 2 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1016/j.bmc.2018.09.015
67210172 169237 0 None -5 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 440 8 1 4 5.3 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2ccccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4166818 169237 0 None -5 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 440 8 1 4 5.3 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2ccccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
67209218 169659 0 None -5 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 406 7 1 4 5.1 CN(C(=O)[C@@H](CC(=O)O)CC1CCCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4173387 169659 0 None -5 2 Mouse 6.8 pEC50 = 6.8 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 406 7 1 4 5.1 CN(C(=O)[C@@H](CC(=O)O)CC1CCCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
67209297 169577 0 None -7 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 422 7 1 5 4.3 CN(C(=O)[C@@H](CC(=O)O)CC1CCOCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4172349 169577 0 None -7 2 Mouse 5.8 pEC50 = 5.8 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 422 7 1 5 4.3 CN(C(=O)[C@@H](CC(=O)O)CC1CCOCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
145952068 169642 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 477 4 1 4 5.1 COc1ccccc1C#Cc1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4173130 169642 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 477 4 1 4 5.1 COc1ccccc1C#Cc1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145950070 169545 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 438 5 1 6 4.3 COc1ccccc1[C@H]1SC[C@@H](C(=O)O)N1C(=O)c1ccc(-c2c(C)noc2C)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4171813 169545 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 438 5 1 6 4.3 COc1ccccc1[C@H]1SC[C@@H](C(=O)O)N1C(=O)c1ccc(-c2c(C)noc2C)cc1 10.1021/acs.jmedchem.8b00855
145949561 169719 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 409 5 1 5 4.3 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccco2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4174384 169719 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 409 5 1 5 4.3 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccco2)cc1 10.1021/acs.jmedchem.8b00855
145954073 169272 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4167352 169272 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
67209297 169577 0 None 7 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 422 7 1 5 4.3 CN(C(=O)[C@@H](CC(=O)O)CC1CCOCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4172349 169577 0 None 7 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 422 7 1 5 4.3 CN(C(=O)[C@@H](CC(=O)O)CC1CCOCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
53302677 169626 1 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 474 8 1 4 5.9 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 10.1021/acs.jmedchem.8b00855
CHEMBL4172928 169626 1 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 474 8 1 4 5.9 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 10.1021/acs.jmedchem.8b00855
145955080 169409 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 465 5 1 4 5.6 CC(=O)c1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4169498 169409 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 465 5 1 4 5.6 CC(=O)c1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
145952174 169777 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 447 3 1 3 5.1 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4175443 169777 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 447 3 1 3 5.1 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
145954381 169354 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 530 6 1 5 6.9 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2c(-c3ccccc3)noc2C2CC2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4168646 169354 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 530 6 1 5 6.9 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2c(-c3ccccc3)noc2C2CC2)cc1 10.1021/acs.jmedchem.8b00855
145962491 169150 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 427 4 1 5 4.1 Cn1nccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4165226 169150 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 427 4 1 5 4.1 Cn1nccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145949561 169719 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 409 5 1 5 4.3 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccco2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4174384 169719 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 409 5 1 5 4.3 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccco2)cc1 10.1021/acs.jmedchem.8b00855
145956912 168831 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 453 5 1 4 5.4 COc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4160351 168831 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 453 5 1 4 5.4 COc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
145952068 169642 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 477 4 1 4 5.1 COc1ccccc1C#Cc1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4173130 169642 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 477 4 1 4 5.1 COc1ccccc1C#Cc1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145959365 168779 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 497 5 1 4 5.5 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Br)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4159447 168779 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 497 5 1 4 5.5 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Br)cc1 10.1021/acs.jmedchem.8b00855
145951076 169752 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 408 4 1 5 4.3 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4175033 169752 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 408 4 1 5 4.3 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
145951986 169483 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4170748 169483 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
67209751 168948 0 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 505 10 1 6 6.0 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC3CCCC3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
CHEMBL4162307 168948 0 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 505 10 1 6 6.0 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC3CCCC3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
117898634 169174 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 479 10 1 6 5.5 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC(C)C)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
CHEMBL4165748 169174 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 479 10 1 6 5.5 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC(C)C)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
117898651 169672 0 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 541 10 1 7 6.2 O=C(O)C[C@@H](CC1CCCC1)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4173663 169672 0 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 541 10 1 7 6.2 O=C(O)C[C@@H](CC1CCCC1)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
117898644 169876 0 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 515 10 1 7 5.7 CC(C)C[C@H](CC(=O)O)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4177037 169876 0 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 515 10 1 7 5.7 CC(C)C[C@H](CC(=O)O)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
46235794 169714 0 None -2 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 414 7 1 4 4.8 CN(C(=O)[C@@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4174307 169714 0 None -2 2 Mouse 6.6 pEC50 = 6.6 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 414 7 1 4 4.8 CN(C(=O)[C@@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
145951986 169483 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4170748 169483 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145952606 169779 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 423 4 1 3 5.3 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1cccc(-c2ccccc2)c1 10.1021/acs.jmedchem.8b00855
CHEMBL4175455 169779 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 423 4 1 3 5.3 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1cccc(-c2ccccc2)c1 10.1021/acs.jmedchem.8b00855
145954073 169272 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4167352 169272 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
145957346 168749 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 419 5 1 4 4.7 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4159019 168749 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 419 5 1 4 4.7 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
67210172 169237 0 None 5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 440 8 1 4 5.3 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2ccccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4166818 169237 0 None 5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 440 8 1 4 5.3 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2ccccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
67209218 169659 0 None 5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 406 7 1 4 5.1 CN(C(=O)[C@@H](CC(=O)O)CC1CCCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4173387 169659 0 None 5 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 406 7 1 4 5.1 CN(C(=O)[C@@H](CC(=O)O)CC1CCCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
145949794 169496 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 414 7 1 4 4.8 CN(C(=O)[C@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4170872 169496 0 None 2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at human FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 414 7 1 4 4.8 CN(C(=O)[C@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
145953603 169259 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 432 4 1 5 4.3 C#Cc1ccccc1[C@H]1SC[C@@H](C(=O)O)N1C(=O)c1ccc(-c2c(C)noc2C)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4167161 169259 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 432 4 1 5 4.3 C#Cc1ccccc1[C@H]1SC[C@@H](C(=O)O)N1C(=O)c1ccc(-c2c(C)noc2C)cc1 10.1021/acs.jmedchem.8b00855
145959365 168779 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 497 5 1 4 5.5 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Br)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4159447 168779 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 497 5 1 4 5.5 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Br)cc1 10.1021/acs.jmedchem.8b00855
145958427 168883 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 409 4 1 6 3.7 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccn2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4161202 168883 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 409 4 1 6 3.7 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccn2)cc1 10.1021/acs.jmedchem.8b00855
138319694 169853 30 None -5 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at mouse FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 442 4 1 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4176503 169853 30 None -5 2 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at mouse FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at mouse FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 442 4 1 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145951370 169560 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 437 4 1 3 5.7 Cc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4171999 169560 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 437 4 1 3 5.7 Cc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145952606 169779 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 423 4 1 3 5.3 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1cccc(-c2ccccc2)c1 10.1021/acs.jmedchem.8b00855
CHEMBL4175455 169779 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 423 4 1 3 5.3 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1cccc(-c2ccccc2)c1 10.1021/acs.jmedchem.8b00855
5803 7182 21 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1021/acs.jmedchem.8b00855
854189 7182 21 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1021/acs.jmedchem.8b00855
CHEMBL594671 7182 21 None -2 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1021/acs.jmedchem.8b00855
145951370 169560 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 437 4 1 3 5.7 Cc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4171999 169560 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 437 4 1 3 5.7 Cc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145956912 168831 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 453 5 1 4 5.4 COc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4160351 168831 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 453 5 1 4 5.4 COc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
145959580 169116 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 443 4 1 4 5.7 Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)s1 10.1021/acs.jmedchem.8b00855
CHEMBL4164813 169116 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 443 4 1 4 5.7 Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)s1 10.1021/acs.jmedchem.8b00855
145949591 169500 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 471 5 1 4 5.5 COc1cccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)c1F 10.1021/acs.jmedchem.8b00855
CHEMBL4170955 169500 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 471 5 1 4 5.5 COc1cccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)c1F 10.1021/acs.jmedchem.8b00855
145951537 169488 0 None -3 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 537 10 1 7 6.0 COc1ccc(-c2ccc(Cl)cc2-c2csc(N(C(=O)[C@@H](CC(=O)O)Cc3ccco3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
CHEMBL4170829 169488 0 None -3 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 537 10 1 7 6.0 COc1ccc(-c2ccc(Cl)cc2-c2csc(N(C(=O)[C@@H](CC(=O)O)Cc3ccco3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
53302677 169626 1 None -1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 474 8 1 4 5.9 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4172928 169626 1 None -1 2 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 474 8 1 4 5.9 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
138319694 169853 30 None -5 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at FFA2R in mouse mature adipocytes assessed as inhibition of isoproterenol-induced glycerol productionAgonist activity at FFA2R in mouse mature adipocytes assessed as inhibition of isoproterenol-induced glycerol production
ChEMBL 442 4 1 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4176503 169853 30 None -5 2 Mouse 5.3 pEC50 = 5.3 Functional
Agonist activity at FFA2R in mouse mature adipocytes assessed as inhibition of isoproterenol-induced glycerol productionAgonist activity at FFA2R in mouse mature adipocytes assessed as inhibition of isoproterenol-induced glycerol production
ChEMBL 442 4 1 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
67258265 169507 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 435 5 1 3 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4171128 169507 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 435 5 1 3 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145952174 169777 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 447 3 1 3 5.1 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4175443 169777 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 447 3 1 3 5.1 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(C#Cc2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
145957026 168987 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4162808 168987 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.8b00855
145958672 168895 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 457 4 1 3 6.0 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4161397 168895 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 457 4 1 3 6.0 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
138319694 169853 30 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 442 4 1 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4176503 169853 30 None 5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 442 4 1 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
117898651 169672 0 None -3 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 541 10 1 7 6.2 O=C(O)C[C@@H](CC1CCCC1)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4173663 169672 0 None -3 2 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 541 10 1 7 6.2 O=C(O)C[C@@H](CC1CCCC1)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
145949794 169496 0 None -2 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 414 7 1 4 4.8 CN(C(=O)[C@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4170872 169496 0 None -2 2 Mouse 6.1 pEC50 = 6.1 Functional
Agonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA methodAgonist activity at mouse FFA2R expressed in CHOK1 cells assessed as induction of GTPgamma35S binding preincubated for 15 mins followed by GTPgamma35S addition measured after 2.5 hrs by SPA method
ChEMBL 414 7 1 4 4.8 CN(C(=O)[C@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
138319694 169853 30 None 5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 442 4 1 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4176503 169853 30 None 5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 442 4 1 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
162648013 186751 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assayAgonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assay
ChEMBL 427 8 1 4 6.3 Cc1nc(-c2ccccc2Cl)sc1COc1cccc([C@@H](CC(=O)O)C2CC2)c1 10.1016/j.bmcl.2020.127460
CHEMBL4746807 186751 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assayAgonist activity at human FFAR2 expressed in HEK293 cells assessed as increase in cAMP level by HTRF assay
ChEMBL 427 8 1 4 6.3 Cc1nc(-c2ccccc2Cl)sc1COc1cccc([C@@H](CC(=O)O)C2CC2)c1 10.1016/j.bmcl.2020.127460
145955080 169409 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 465 5 1 4 5.6 CC(=O)c1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4169498 169409 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 465 5 1 4 5.6 CC(=O)c1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)cc1 10.1021/acs.jmedchem.8b00855
145953626 169290 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 423 4 1 3 5.3 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4167577 169290 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 423 4 1 3 5.3 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
145950070 169545 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 438 5 1 6 4.3 COc1ccccc1[C@H]1SC[C@@H](C(=O)O)N1C(=O)c1ccc(-c2c(C)noc2C)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4171813 169545 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 438 5 1 6 4.3 COc1ccccc1[C@H]1SC[C@@H](C(=O)O)N1C(=O)c1ccc(-c2c(C)noc2C)cc1 10.1021/acs.jmedchem.8b00855
145958672 168895 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 457 4 1 3 6.0 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4161397 168895 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 457 4 1 3 6.0 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145949591 169500 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 471 5 1 4 5.5 COc1cccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)c1F 10.1021/acs.jmedchem.8b00855
CHEMBL4170955 169500 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 471 5 1 4 5.5 COc1cccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)c1F 10.1021/acs.jmedchem.8b00855
145959580 169116 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 443 4 1 4 5.7 Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)s1 10.1021/acs.jmedchem.8b00855
CHEMBL4164813 169116 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 443 4 1 4 5.7 Cc1ccc(-c2ccc(C(=O)N3[C@H](C(=O)O)CS[C@@H]3c3ccccc3Cl)cc2)s1 10.1021/acs.jmedchem.8b00855
145957346 168749 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 419 5 1 4 4.7 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4159019 168749 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assayAgonist activity at human FFA2R expressed in Flp-InT-REx 293 cells assessed as reduction of forskolin-induced cAMP production after 30 mins by TR-FRET assay
ChEMBL 419 5 1 4 4.7 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
145962491 169150 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 427 4 1 5 4.1 Cn1nccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4165226 169150 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assayAgonist activity to human FFA2R expressed in HEK293T cells assessed as induction beta-arrestin-2 recruitment after 10 mins by BRET assay
ChEMBL 427 4 1 5 4.1 Cn1nccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
46226274 209100 0 None - 1 Human 6.0 pIC50 = 6 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 342 3 1 3 5.2 CC(C)(C)[C@H](C(=O)Nc1ncc(Cl)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL610333 209100 0 None - 1 Human 6.0 pIC50 = 6 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 342 3 1 3 5.2 CC(C)(C)[C@H](C(=O)Nc1ncc(Cl)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
118719384 122302 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 384 5 1 2 3.8 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)NCc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3352999 122302 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 384 5 1 2 3.8 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)NCc2ccc(Cl)cc2)c1 10.1021/jm5012885
68175794 122307 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 427 7 1 3 3.5 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCN)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353004 122307 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 427 7 1 3 3.5 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCN)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
118719385 122308 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 2 3 3.4 CNC(=O)NCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
CHEMBL3353005 122308 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 2 3 3.4 CNC(=O)NCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
46226177 206548 0 None - 1 Human 4.0 pIC50 = 4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 279 4 2 4 2.2 CC(C)C(C(=O)Nc1nnn[nH]1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593826 206548 0 None - 1 Human 4.0 pIC50 = 4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 279 4 2 4 2.2 CC(C)C(C(=O)Nc1nnn[nH]1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226178 206549 0 None - 1 Human 4.0 pIC50 = 4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 277 4 2 2 3.4 CC(C)[C@H](C(=O)Nc1cc[nH]n1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593827 206549 0 None - 1 Human 4.0 pIC50 = 4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 277 4 2 2 3.4 CC(C)[C@H](C(=O)Nc1cc[nH]n1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
847243 206697 12 None - 1 Human 4.0 pIC50 = 4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 252 3 1 3 3.0 O=C(Cc1ccc(Cl)cc1)Nc1nccs1 10.1016/j.bmcl.2009.11.112
CHEMBL594760 206697 12 None - 1 Human 4.0 pIC50 = 4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 252 3 1 3 3.0 O=C(Cc1ccc(Cl)cc1)Nc1nccs1 10.1016/j.bmcl.2009.11.112
46226356 206691 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 292 5 1 3 4.1 C=CC[C@H](C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594738 206691 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 292 5 1 3 4.1 C=CC[C@H](C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226144 206694 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 306 4 1 2 4.3 CC(C)[C@H](C(=O)Nc1cccc(F)n1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594746 206694 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 306 4 1 2 4.3 CC(C)[C@H](C(=O)Nc1cccc(F)n1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226383 208846 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 344 4 1 3 4.4 O=C(Nc1ncc(F)s1)[C@H](c1ccc(C(F)(F)F)cc1)C1CC1 10.1016/j.bmcl.2009.11.112
CHEMBL608697 208846 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 344 4 1 3 4.4 O=C(Nc1ncc(F)s1)[C@H](c1ccc(C(F)(F)F)cc1)C1CC1 10.1016/j.bmcl.2009.11.112
46226106 206901 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 225 3 1 1 2.8 CNC(=O)[C@H](c1ccc(Cl)cc1)C(C)C 10.1016/j.bmcl.2009.11.112
CHEMBL596153 206901 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 225 3 1 1 2.8 CNC(=O)[C@H](c1ccc(Cl)cc1)C(C)C 10.1016/j.bmcl.2009.11.112
77904272 122409 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 498 9 1 4 5.1 CC1(C(=O)N(CCCC(=O)O)CCc2ccc(Cl)cc2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353510 122409 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 498 9 1 4 5.1 CC1(C(=O)N(CCCC(=O)O)CCc2ccc(Cl)cc2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
70558275 122415 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 490 8 1 5 5.1 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3ccoc3c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353516 122415 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 490 8 1 5 5.1 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3ccoc3c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
89894240 122436 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 488 9 1 5 4.6 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3ccoc3c2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
CHEMBL3353539 122436 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 488 9 1 5 4.6 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3ccoc3c2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
70559113 122407 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 1 4 5.1 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353502 122407 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 1 4 5.1 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
46226336 206734 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 310 4 1 3 4.1 O=C(Nc1ncc(F)s1)[C@H](c1ccc(Cl)cc1)C1CC1 10.1016/j.bmcl.2009.11.112
CHEMBL594998 206734 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 310 4 1 3 4.1 O=C(Nc1ncc(F)s1)[C@H](c1ccc(Cl)cc1)C1CC1 10.1016/j.bmcl.2009.11.112
46226312 208524 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 474 4 2 4 5.9 CC(C)(C)[C@H](C(=O)Nc1ncc(C(O)(C(F)(F)F)C(F)(F)F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL606629 208524 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 474 4 2 4 5.9 CC(C)(C)[C@H](C(=O)Nc1ncc(C(O)(C(F)(F)F)C(F)(F)F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
29369661 206661 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 295 4 1 4 3.6 CC(C)[C@H](C(=O)Nc1nncs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594537 206661 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 295 4 1 4 3.6 CC(C)[C@H](C(=O)Nc1nncs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
68176091 122375 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 442 8 0 3 4.2 COCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
CHEMBL3353464 122375 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 442 8 0 3 4.2 COCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
70556816 122379 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 441 7 1 3 3.0 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CC(N)=O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353468 122379 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 441 7 1 3 3.0 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CC(N)=O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
70561343 122416 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 490 8 2 5 4.3 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cn[nH]c3c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353517 122416 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 490 8 2 5 4.3 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cn[nH]c3c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
46226145 208972 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 306 4 1 2 4.3 CC(C)[C@H](C(=O)Nc1ccc(F)cn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL609584 208972 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 306 4 1 2 4.3 CC(C)[C@H](C(=O)Nc1ccc(F)cn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70561241 122437 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 488 9 2 5 3.7 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cn[nH]c3c2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
CHEMBL3353540 122437 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 488 9 2 5 3.7 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cn[nH]c3c2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
46226143 206693 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 288 4 1 2 4.1 CC(C)[C@H](C(=O)Nc1ccccn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594745 206693 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 288 4 1 2 4.1 CC(C)[C@H](C(=O)Nc1ccccn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
9095896 206845 2 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 308 4 1 3 4.5 Cc1csc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)C)n1 10.1016/j.bmcl.2009.11.112
CHEMBL595715 206845 2 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 308 4 1 3 4.5 Cc1csc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)C)n1 10.1016/j.bmcl.2009.11.112
68175951 122404 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 412 4 0 3 4.8 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353498 122404 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 412 4 0 3 4.8 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
89900352 122377 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 479 8 0 4 5.4 CC1(C(=O)N(CCCC#N)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353466 122377 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 479 8 0 4 5.4 CC1(C(=O)N(CCCC#N)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
89900321 122303 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 398 5 0 2 4.1 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(C)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353000 122303 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 398 5 0 2 4.1 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(C)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
70556487 122301 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 412 5 1 3 4.4 CC1(C(=O)NCc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3352998 122301 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 412 5 1 3 4.4 CC1(C(=O)NCc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
46226360 208938 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 310 3 1 3 4.0 O=C(Nc1ncc(F)s1)C1(c2ccc(Cl)cc2)CCC1 10.1016/j.bmcl.2009.11.112
CHEMBL609291 208938 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 310 3 1 3 4.0 O=C(Nc1ncc(F)s1)C1(c2ccc(Cl)cc2)CCC1 10.1016/j.bmcl.2009.11.112
46226254 209010 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 362 4 1 3 5.2 CC(C)[C@H](C(=O)Nc1ncc(C(F)(F)F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL609861 209010 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 362 4 1 3 5.2 CC(C)[C@H](C(=O)Nc1ncc(C(F)(F)F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226290 209011 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 333 3 1 4 4.4 CC(C)(C)[C@H](C(=O)Nc1ncc(C#N)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL609863 209011 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 333 3 1 4 4.4 CC(C)(C)[C@H](C(=O)Nc1ncc(C#N)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226291 209275 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 376 3 1 3 5.6 CC(C)(C)[C@H](C(=O)Nc1ncc(C(F)(F)F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL611340 209275 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 376 3 1 3 5.6 CC(C)(C)[C@H](C(=O)Nc1ncc(C(F)(F)F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70565254 122426 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 476 9 2 4 3.6 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc3cn[nH]c3c2)c1 10.1021/jm5012885
CHEMBL3353528 122426 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 476 9 2 4 3.6 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc3cn[nH]c3c2)c1 10.1021/jm5012885
68176356 122382 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 469 9 1 3 3.8 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(N)=O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353471 122382 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 469 9 1 3 3.8 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(N)=O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
68176096 122381 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 469 7 0 3 3.6 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CC(=O)N(C)C)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353470 122381 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 469 7 0 3 3.6 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CC(=O)N(C)C)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
46226308 206690 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 351 4 1 4 4.6 CN(C)c1cnc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)(C)C)s1 10.1016/j.bmcl.2009.11.112
CHEMBL594737 206690 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 351 4 1 4 4.6 CN(C)c1cnc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)(C)C)s1 10.1016/j.bmcl.2009.11.112
46226309 208068 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 393 4 1 5 4.4 CC(C)(C)[C@H](C(=O)Nc1ncc(N2CCOCC2)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL604059 208068 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 393 4 1 5 4.4 CC(C)(C)[C@H](C(=O)Nc1ncc(N2CCOCC2)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226385 206775 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 311 4 1 4 3.5 O=C(Nc1ncc(F)s1)[C@H](c1ccnc(Cl)c1)C1CC1 10.1016/j.bmcl.2009.11.112
CHEMBL595235 206775 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 311 4 1 4 3.5 O=C(Nc1ncc(F)s1)[C@H](c1ccnc(Cl)c1)C1CC1 10.1016/j.bmcl.2009.11.112
89894379 140239 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 482 9 1 4 4.5 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
CHEMBL3706688 140239 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 482 9 1 4 4.5 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
46226235 208901 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 362 4 1 3 5.2 CC(C)[C@H](C(=O)Nc1nc(C(F)(F)F)cs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL608991 208901 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 362 4 1 3 5.2 CC(C)[C@H](C(=O)Nc1nc(C(F)(F)F)cs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70556496 122421 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 470 9 1 3 4.4 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353523 122421 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 470 9 1 3 4.4 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
46226251 209176 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 322 4 1 3 4.8 Cc1nc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)C)sc1C 10.1016/j.bmcl.2009.11.112
CHEMBL610741 209176 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 322 4 1 3 4.8 Cc1nc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)C)sc1C 10.1016/j.bmcl.2009.11.112
36477073 206703 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 363 4 1 4 4.6 CC(C)[C@H](C(=O)Nc1nnc(C(F)(F)F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594770 206703 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 363 4 1 4 4.6 CC(C)[C@H](C(=O)Nc1nnc(C(F)(F)F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226255 206554 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 319 4 1 4 4.0 CC(C)[C@H](C(=O)Nc1ncc(C#N)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593839 206554 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 319 4 1 4 4.0 CC(C)[C@H](C(=O)Nc1ncc(C#N)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
39725404 206647 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 352 5 1 5 4.0 COC(=O)c1cnc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)C)s1 10.1016/j.bmcl.2009.11.112
CHEMBL594505 206647 1 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 352 5 1 5 4.0 COC(=O)c1cnc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)C)s1 10.1016/j.bmcl.2009.11.112
46226163 206704 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 295 4 1 4 3.6 CC(C)[C@H](C(=O)Nc1ncns1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594771 206704 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 295 4 1 4 3.6 CC(C)[C@H](C(=O)Nc1ncns1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
135971436 206461 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 310 3 1 3 2.8 CC(C)[C@H](C(=O)NC1=NC(=O)CS1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593121 206461 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 310 3 1 3 2.8 CC(C)[C@H](C(=O)NC1=NC(=O)CS1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226164 206529 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 277 4 2 2 3.4 CC(C)[C@H](C(=O)Nc1ncc[nH]1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593607 206529 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 277 4 2 2 3.4 CC(C)[C@H](C(=O)Nc1ncc[nH]1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
2520490 206460 2 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 296 3 1 3 3.3 CC(C)[C@H](C(=O)NC1=NCCS1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593120 206460 2 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 296 3 1 3 3.3 CC(C)[C@H](C(=O)NC1=NCCS1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
89894269 140240 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 454 7 1 4 3.7 CC1(C(=O)N(CC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
CHEMBL3706689 140240 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 454 7 1 4 3.7 CC1(C(=O)N(CC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
46226161 206500 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 289 4 1 3 3.5 CC(C)[C@H](C(=O)Nc1cccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593435 206500 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 289 4 1 3 3.5 CC(C)[C@H](C(=O)Nc1cccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226311 206649 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 441 4 1 6 3.8 CC(C)(C)[C@H](C(=O)Nc1ncc(N2CCS(=O)(=O)CC2)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594507 206649 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 441 4 1 6 3.8 CC(C)(C)[C@H](C(=O)Nc1ncc(N2CCS(=O)(=O)CC2)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
68176357 122389 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 505 9 1 4 3.2 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCS(N)(=O)=O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353478 122389 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 505 9 1 4 3.2 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCS(N)(=O)=O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
89900347 122376 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 451 6 0 4 4.6 CC1(C(=O)N(CC#N)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353465 122376 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 451 6 0 4 4.6 CC1(C(=O)N(CC#N)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
70559604 122413 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 1 4 5.1 CC1(C(=O)N(CCCC(=O)O)Cc2cccc(Cl)c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353514 122413 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 1 4 5.1 CC1(C(=O)N(CCCC(=O)O)Cc2cccc(Cl)c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
46226162 206501 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 278 4 1 3 3.7 CC(C)[C@H](C(=O)Nc1ncco1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593436 206501 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 278 4 1 3 3.7 CC(C)[C@H](C(=O)Nc1ncco1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226295 206586 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 432 5 1 3 6.8 CC(C)(C)[C@H](C(=O)Nc1ncc(Cc2ccc(Cl)cc2)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594074 206586 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 432 5 1 3 6.8 CC(C)(C)[C@H](C(=O)Nc1ncc(Cc2ccc(Cl)cc2)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70559551 122412 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 518 8 1 4 5.4 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(C(F)(F)F)cc2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353513 122412 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 518 8 1 4 5.4 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(C(F)(F)F)cc2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
89894353 122434 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 516 9 1 4 4.9 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(C(F)(F)F)cc2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
CHEMBL3353536 122434 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 516 9 1 4 4.9 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(C(F)(F)F)cc2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
89900371 122393 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 519 10 1 4 3.5 CNS(=O)(=O)CCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
CHEMBL3353481 122393 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 519 10 1 4 3.5 CNS(=O)(=O)CCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
89900327 122304 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 426 5 0 3 4.7 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353001 122304 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 426 5 0 3 4.7 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
70558376 122394 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 442 7 1 3 3.6 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CC(=O)O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353482 122394 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 442 7 1 3 3.6 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CC(=O)O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
88757504 122420 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 471 7 1 5 4.5 CC1(C(=O)N(CCCC(=O)O)c2ccc(Cl)nc2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353522 122420 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 471 7 1 5 4.5 CC1(C(=O)N(CCCC(=O)O)c2ccc(Cl)nc2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
46226182 209009 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 344 4 1 3 5.3 CC(C)C(C(=O)Nc1nc2ccccc2s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL609852 209009 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 344 4 1 3 5.3 CC(C)C(C(=O)Nc1nc2ccccc2s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70558485 122396 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 1 4 4.6 CC1(C(=O)N(CCC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353484 122396 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 1 4 4.6 CC1(C(=O)N(CCC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
70557254 122417 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 507 8 1 6 5.0 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3scnc3c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353518 122417 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 507 8 1 6 5.0 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3scnc3c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
118719612 122290 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 426 5 0 4 4.3 COc1c(C(=O)N2CCC2(C)C(=O)N(C)Cc2ccc(Cl)cc2)csc1Cl 10.1021/jm5012885
CHEMBL3352828 122290 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 426 5 0 4 4.3 COc1c(C(=O)N2CCC2(C)C(=O)N(C)Cc2ccc(Cl)cc2)csc1Cl 10.1021/jm5012885
68176101 122306 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 456 7 1 4 4.1 CC1(C(=O)N(CCO)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353003 122306 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 456 7 1 4 4.1 CC1(C(=O)N(CCO)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
118719611 122401 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 406 4 0 2 4.8 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)c1cccc2ccccc12 10.1021/jm5012885
CHEMBL3353491 122401 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 406 4 0 2 4.8 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)c1cccc2ccccc12 10.1021/jm5012885
118719617 122405 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 446 4 0 3 5.5 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)c1csc2ccc(Cl)cc12 10.1021/jm5012885
CHEMBL3353499 122405 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 446 4 0 3 5.5 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)c1csc2ccc(Cl)cc12 10.1021/jm5012885
70557757 122423 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 470 9 1 3 4.4 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2cccc(Cl)c2)c1 10.1021/jm5012885
CHEMBL3353525 122423 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 470 9 1 3 4.4 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2cccc(Cl)c2)c1 10.1021/jm5012885
118719609 122387 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 497 8 1 4 4.3 CC(=O)NCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353476 122387 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 497 8 1 4 4.3 CC(=O)NCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
46226293 208973 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 386 4 1 5 4.0 CC(C)(C)[C@H](C(=O)Nc1ncc(S(C)(=O)=O)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL609586 208973 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 386 4 1 5 4.0 CC(C)(C)[C@H](C(=O)Nc1ncc(S(C)(=O)=O)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70556905 122411 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 470 7 1 4 5.1 CC1(C(=O)N(CCCC(=O)O)c2cccc(Cl)c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353512 122411 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 470 7 1 4 5.1 CC1(C(=O)N(CCCC(=O)O)c2cccc(Cl)c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
70556713 122395 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 470 7 1 4 4.2 CC1(C(=O)N(CC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353483 122395 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 470 7 1 4 4.2 CC1(C(=O)N(CC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
70559086 122431 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 504 9 1 5 5.1 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3ccoc3c2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353533 122431 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 504 9 1 5 5.1 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3ccoc3c2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
46226179 208810 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 278 4 1 3 3.7 CC(C)[C@H](C(=O)Nc1ccon1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL608384 208810 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 278 4 1 3 3.7 CC(C)[C@H](C(=O)Nc1ccon1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70559096 122378 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 9 0 4 4.5 COC(=O)CCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
CHEMBL3353467 122378 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 9 0 4 4.5 COC(=O)CCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
46226310 206648 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 406 4 1 5 4.3 CN1CCN(c2cnc(NC(=O)[C@H](c3ccc(Cl)cc3)C(C)(C)C)s2)CC1 10.1016/j.bmcl.2009.11.112
CHEMBL594506 206648 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 406 4 1 5 4.3 CN1CCN(c2cnc(NC(=O)[C@H](c3ccc(Cl)cc3)C(C)(C)C)s2)CC1 10.1016/j.bmcl.2009.11.112
89900361 122385 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 539 9 0 4 4.2 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)N2CCOCC2)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353474 122385 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 539 9 0 4 4.2 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)N2CCOCC2)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
70562777 122432 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 504 9 2 5 4.2 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cn[nH]c3c2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353534 122432 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 504 9 2 5 4.2 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cn[nH]c3c2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
70557843 122397 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 498 9 1 4 5.0 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353485 122397 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 498 9 1 4 5.0 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
68175817 122388 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 505 9 1 4 3.1 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCNS(C)(=O)=O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353477 122388 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 505 9 1 4 3.1 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCNS(C)(=O)=O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
46226234 209175 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 362 4 1 3 5.5 CC(C)[C@H](C(=O)Nc1nc2cc(Cl)ccc2o1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL610740 209175 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 362 4 1 3 5.5 CC(C)[C@H](C(=O)Nc1nc2cc(Cl)ccc2o1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
89901463 122392 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 547 10 1 5 4.1 CNS(=O)(=O)CCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353480 122392 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 547 10 1 5 4.1 CNS(=O)(=O)CCCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
68176095 122380 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 455 7 1 3 3.3 CNC(=O)CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
CHEMBL3353469 122380 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 455 7 1 3 3.3 CNC(=O)CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
89900348 122402 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 423 5 0 3 4.0 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cn(C)c2ccccc12 10.1021/jm5012885
CHEMBL3353492 122402 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 423 5 0 3 4.0 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cn(C)c2ccccc12 10.1021/jm5012885
46226386 206655 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 277 4 1 4 2.8 O=C(Nc1ncc(F)s1)[C@H](c1ccccn1)C1CC1 10.1016/j.bmcl.2009.11.112
CHEMBL594528 206655 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 277 4 1 4 2.8 O=C(Nc1ncc(F)s1)[C@H](c1ccccn1)C1CC1 10.1016/j.bmcl.2009.11.112
46226333 206698 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 266 3 1 3 3.5 C[C@H](C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594761 206698 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 266 3 1 3 3.5 C[C@H](C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
89900346 122384 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 511 7 0 4 3.4 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CC(=O)N2CCOCC2)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353473 122384 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 511 7 0 4 3.4 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CC(=O)N2CCOCC2)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
68176013 122305 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 412 6 0 2 4.5 CCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
CHEMBL3353002 122305 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 412 6 0 2 4.5 CCN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(C)cc(C)c1 10.1021/jm5012885
70564780 122430 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 503 9 2 4 4.8 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cc[nH]c3c2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353532 122430 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 503 9 2 4 4.8 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cc[nH]c3c2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
46226142 206692 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 288 4 1 2 4.1 CC(C)C(C(=O)Nc1cccnc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594744 206692 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 288 4 1 2 4.1 CC(C)C(C(=O)Nc1cccnc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
3420 10221 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 312 4 1 3 4.3 CC([C@H](C(=O)Nc1ncc(s1)F)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2009.11.112
46226252 10221 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 312 4 1 3 4.3 CC([C@H](C(=O)Nc1ncc(s1)F)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2009.11.112
CHEMBL594525 10221 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 312 4 1 3 4.3 CC([C@H](C(=O)Nc1ncc(s1)F)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2009.11.112
46226292 206696 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 354 4 1 4 5.3 CSc1cnc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)(C)C)s1 10.1016/j.bmcl.2009.11.112
CHEMBL594758 206696 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 354 4 1 4 5.3 CSc1cnc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)(C)C)s1 10.1016/j.bmcl.2009.11.112
70557810 122429 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 498 9 1 4 5.0 CC1(C(=O)N(CCCC(=O)O)Cc2cccc(Cl)c2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353531 122429 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 498 9 1 4 5.0 CC1(C(=O)N(CCCC(=O)O)Cc2cccc(Cl)c2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
46226361 206728 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 324 3 1 3 4.4 O=C(Nc1ncc(F)s1)C1(c2ccc(Cl)cc2)CCCC1 10.1016/j.bmcl.2009.11.112
CHEMBL594974 206728 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 324 3 1 3 4.4 O=C(Nc1ncc(F)s1)C1(c2ccc(Cl)cc2)CCCC1 10.1016/j.bmcl.2009.11.112
46226334 209012 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 280 4 1 3 3.9 CC[C@H](C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL609870 209012 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 280 4 1 3 3.9 CC[C@H](C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226358 209367 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 298 3 1 3 3.9 CC(C)(C(=O)Nc1ncc(F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL611948 209367 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 298 3 1 3 3.9 CC(C)(C(=O)Nc1ncc(F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
89900356 122406 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 426 5 0 3 4.7 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc2ccccc2s1 10.1021/jm5012885
CHEMBL3353500 122406 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 426 5 0 3 4.7 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc2ccccc2s1 10.1021/jm5012885
70556743 122408 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 455 7 1 5 3.1 CC1(C(=O)N(CC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1noc2ccccc12 10.1021/jm5012885
CHEMBL3353505 122408 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 455 7 1 5 3.1 CC1(C(=O)N(CC(=O)O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1noc2ccccc12 10.1021/jm5012885
70558482 122403 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 396 4 0 3 4.3 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)c1ccc2occc2c1 10.1021/jm5012885
CHEMBL3353495 122403 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 396 4 0 3 4.3 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)c1ccc2occc2c1 10.1021/jm5012885
68176100 122383 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 455 8 1 3 3.4 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCC(N)=O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
CHEMBL3353472 122383 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 455 8 1 3 3.4 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCC(N)=O)Cc2ccc(Cl)cc2)c1 10.1021/jm5012885
4964042 209054 4 None - 1 Human 5.3 pIC50 = 5.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 327 4 2 2 4.6 CC(C)C(C(=O)Nc1nc2ccccc2[nH]1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL610060 209054 4 None - 1 Human 5.3 pIC50 = 5.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 327 4 2 2 4.6 CC(C)C(C(=O)Nc1nc2ccccc2[nH]1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226146 206491 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 289 4 1 3 3.5 CC(C)C(C(=O)Nc1ncccn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593351 206491 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 289 4 1 3 3.5 CC(C)C(C(=O)Nc1ncccn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226335 206699 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 294 5 1 3 4.3 CCC[C@H](C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594762 206699 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 294 5 1 3 4.3 CCC[C@H](C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70559021 122422 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 504 9 1 3 4.7 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc(C(F)(F)F)cc2)c1 10.1021/jm5012885
CHEMBL3353524 122422 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 504 9 1 3 4.7 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc(C(F)(F)F)cc2)c1 10.1021/jm5012885
25479840 206498 1 None - 1 Human 4.3 pIC50 = 4.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 288 4 1 2 4.1 CC(C)[C@H](C(=O)Nc1ccncc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593433 206498 1 None - 1 Human 4.3 pIC50 = 4.3 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 288 4 1 2 4.1 CC(C)[C@H](C(=O)Nc1ccncc1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70557930 122428 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 532 9 1 4 5.3 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(C(F)(F)F)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353530 122428 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 532 9 1 4 5.3 CC1(C(=O)N(CCCC(=O)O)Cc2ccc(C(F)(F)F)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
46226160 209322 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 289 4 1 3 3.5 CC(C)C(C(=O)Nc1cnccn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL611632 209322 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 289 4 1 3 3.5 CC(C)C(C(=O)Nc1cnccn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226180 206961 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 295 4 1 4 3.6 CC(C)[C@H](C(=O)Nc1cnns1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL596580 206961 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 295 4 1 4 3.6 CC(C)[C@H](C(=O)Nc1cnns1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70559585 122418 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 471 7 1 5 4.5 CC1(C(=O)N(CCCC(=O)O)c2cc(Cl)ccn2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353520 122418 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 471 7 1 5 4.5 CC1(C(=O)N(CCCC(=O)O)c2cc(Cl)ccn2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
118719610 122400 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 452 6 0 3 5.3 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cccc(-c2ccsc2)c1 10.1021/jm5012885
CHEMBL3353490 122400 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 452 6 0 3 5.3 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cccc(-c2ccsc2)c1 10.1021/jm5012885
46226337 208845 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 308 5 1 3 4.6 CC(C)C[C@H](C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL608696 208845 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 308 5 1 3 4.6 CC(C)C[C@H](C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70557795 122410 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 470 7 1 4 5.1 CC1(C(=O)N(CCCC(=O)O)c2ccc(Cl)cc2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353511 122410 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 470 7 1 4 5.1 CC1(C(=O)N(CCCC(=O)O)c2ccc(Cl)cc2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
70564643 122414 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 489 8 2 4 4.9 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cc[nH]c3c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353515 122414 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 489 8 2 4 4.9 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cc[nH]c3c2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
70559574 122419 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 471 7 1 5 4.5 CC1(C(=O)N(CCCC(=O)O)c2ccc(Cl)cn2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
CHEMBL3353521 122419 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 471 7 1 5 4.5 CC1(C(=O)N(CCCC(=O)O)c2ccc(Cl)cn2)CCN1C(=O)c1csc2ccccc12 10.1021/jm5012885
5803 7182 21 None -2 2 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2009.11.112
854189 7182 21 None -2 2 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2009.11.112
CHEMBL594671 7182 21 None -2 2 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 10.1016/j.bmcl.2009.11.112
12861 7982 26 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 384 4 1 3 6.2 CC(C)(C)[C@@H](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 10.1016/j.bmcl.2009.11.112
46226294 7982 26 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 384 4 1 3 6.2 CC(C)(C)[C@@H](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 10.1016/j.bmcl.2009.11.112
CHEMBL607315 7982 26 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 384 4 1 3 6.2 CC(C)(C)[C@@H](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 10.1016/j.bmcl.2009.11.112
46226275 206488 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 386 3 1 3 5.3 CC(C)(C)[C@H](C(=O)Nc1ncc(Br)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593344 206488 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 386 3 1 3 5.3 CC(C)(C)[C@H](C(=O)Nc1ncc(Br)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226273 209273 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 326 3 1 3 4.7 CC(C)(C)[C@H](C(=O)Nc1ncc(F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL611338 209273 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 326 3 1 3 4.7 CC(C)(C)[C@H](C(=O)Nc1ncc(F)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226253 209274 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 328 4 1 3 4.8 CC(C)[C@H](C(=O)Nc1ncc(Cl)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL611339 209274 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 328 4 1 3 4.8 CC(C)[C@H](C(=O)Nc1ncc(Cl)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226272 208715 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 337 5 2 4 3.3 CC(C)[C@H](C(=O)Nc1ncc(C(N)=O)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL607691 208715 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 337 5 2 4 3.3 CC(C)[C@H](C(=O)Nc1ncc(C(N)=O)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70559626 122427 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 493 9 1 5 4.3 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc3scnc3c2)c1 10.1021/jm5012885
CHEMBL3353529 122427 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 493 9 1 5 4.3 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc3scnc3c2)c1 10.1021/jm5012885
89900365 122386 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 567 9 0 5 4.8 CC1(C(=O)N(CCCC(=O)N2CCOCC2)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353475 122386 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 567 9 0 5 4.8 CC1(C(=O)N(CCCC(=O)N2CCOCC2)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
89900378 122390 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 533 9 1 5 3.8 CC1(C(=O)N(CCCS(N)(=O)=O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353479 122390 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 533 9 1 5 3.8 CC1(C(=O)N(CCCS(N)(=O)=O)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
68175329 122399 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 446 6 0 2 5.2 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cccc(-c2ccccc2)c1 10.1021/jm5012885
CHEMBL3353489 122399 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 446 6 0 2 5.2 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cccc(-c2ccccc2)c1 10.1021/jm5012885
70558983 122425 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 476 9 1 4 4.5 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc3ccoc3c2)c1 10.1021/jm5012885
CHEMBL3353527 122425 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 476 9 1 4 4.5 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc3ccoc3c2)c1 10.1021/jm5012885
68175946 122398 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 406 5 0 2 3.8 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(F)cc(F)c1 10.1021/jm5012885
CHEMBL3353487 122398 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 406 5 0 2 3.8 CN(Cc1ccc(Cl)cc1)C(=O)C1(C)CCN1C(=O)Cc1cc(F)cc(F)c1 10.1021/jm5012885
46226236 206581 1 None - 1 Human 5.1 pIC50 = 5.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 350 4 1 3 5.5 CC(C)[C@H](C(=O)Nc1nc(C(C)(C)C)cs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594052 206581 1 None - 1 Human 5.1 pIC50 = 5.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 350 4 1 3 5.5 CC(C)[C@H](C(=O)Nc1nc(C(C)(C)C)cs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226271 206595 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 338 5 2 4 3.9 CC(C)[C@H](C(=O)Nc1ncc(C(=O)O)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594140 206595 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 338 5 2 4 3.9 CC(C)[C@H](C(=O)Nc1ncc(C(=O)O)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
2397905 206653 2 None - 1 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 308 4 1 3 4.5 Cc1cnc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)C)s1 10.1016/j.bmcl.2009.11.112
CHEMBL594524 206653 2 None - 1 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 308 4 1 3 4.5 Cc1cnc(NC(=O)[C@H](c2ccc(Cl)cc2)C(C)C)s1 10.1016/j.bmcl.2009.11.112
4307629 209120 47 None - 1 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 294 4 1 3 4.2 CC(C)C(C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL610463 209120 47 None - 1 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 294 4 1 3 4.2 CC(C)C(C(=O)Nc1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46225340 206535 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 308 4 0 3 4.2 CC(C)[C@H](C(=O)N(C)c1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL593733 206535 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 308 4 0 3 4.2 CC(C)[C@H](C(=O)N(C)c1nccs1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
70562873 122424 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 475 9 2 3 4.2 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc3cc[nH]c3c2)c1 10.1021/jm5012885
CHEMBL3353526 122424 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 475 9 2 3 4.2 Cc1cc(C)cc(CC(=O)N2CCC2(C)C(=O)N(CCCC(=O)O)Cc2ccc3cc[nH]c3c2)c1 10.1021/jm5012885
46226382 206737 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 338 3 1 3 4.8 O=C(Nc1ncc(F)s1)C1(c2ccc(Cl)cc2)CCCCC1 10.1016/j.bmcl.2009.11.112
CHEMBL595000 206737 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 338 3 1 3 4.8 O=C(Nc1ncc(F)s1)C1(c2ccc(Cl)cc2)CCCCC1 10.1016/j.bmcl.2009.11.112
46226338 206622 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 306 5 1 3 4.3 O=C(Nc1nccs1)[C@@H](CC1CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL594302 206622 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 306 5 1 3 4.3 O=C(Nc1nccs1)[C@@H](CC1CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
57520598 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/jm5012885
8417 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/jm5012885
CHEMBL3353541 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/jm5012885
DB15406 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/jm5012885
70566934 122435 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 487 9 2 4 4.3 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cc[nH]c3c2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
CHEMBL3353538 122435 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 487 9 2 4 4.3 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3cc[nH]c3c2)CCN1C(=O)Cc1coc2ccccc12 10.1021/jm5012885
70556909 122433 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 521 9 1 6 4.9 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3scnc3c2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353535 122433 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilizationAntagonist activity against human FFA2 receptor expressed in HEK293 cells assessed as inhibition of sodium acetate-induced calcium mobilization
ChEMBL 521 9 1 6 4.9 CC1(C(=O)N(CCCC(=O)O)Cc2ccc3scnc3c2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
1058 7042 85 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
176 7042 85 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
21980959 7042 85 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
4211 7042 85 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
CHEMBL539 7042 85 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
DB03166 7042 85 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
10107 10655 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity in a BRET-based β-arrestin-2 recruitment assay.Agonist activity in a BRET-based β-arrestin-2 recruitment assay.
Guide to Pharmacology 442 4 1 5 5.0 O=C(N1[C@H](CS[C@H]1c1ccccc1Cl)C(=O)O)c1ccc(cc1)c1c(C)noc1C 30247908
137321147 10655 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity in a BRET-based β-arrestin-2 recruitment assay.Agonist activity in a BRET-based β-arrestin-2 recruitment assay.
Guide to Pharmacology 442 4 1 5 5.0 O=C(N1[C@H](CS[C@H]1c1ccccc1Cl)C(=O)O)c1ccc(cc1)c1c(C)noc1C 30247908
10107 10655 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity in a cAMP inhibition assay.Agonist activity in a cAMP inhibition assay.
Guide to Pharmacology 442 4 1 5 5.0 O=C(N1[C@H](CS[C@H]1c1ccccc1Cl)C(=O)O)c1ccc(cc1)c1c(C)noc1C 30247908
137321147 10655 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity in a cAMP inhibition assay.Agonist activity in a cAMP inhibition assay.
Guide to Pharmacology 442 4 1 5 5.0 O=C(N1[C@H](CS[C@H]1c1ccccc1Cl)C(=O)O)c1ccc(cc1)c1c(C)noc1C 30247908
6500 6823 115 None -47 2 Human 2.6 pEC50 = 2.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 100 1 1 1 0.9 OC(=O)C1(C)CC1 21220428
81326 6823 115 None -47 2 Human 2.6 pEC50 = 2.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 100 1 1 1 0.9 OC(=O)C1(C)CC1 21220428
CHEMBL4516837 6823 115 None -47 2 Human 2.6 pEC50 = 2.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 100 1 1 1 0.9 OC(=O)C1(C)CC1 21220428
1061 9818 0 None -50 2 Human 2.9 pEC50 = 2.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 102 3 1 1 1.3 CCCCC(=O)O 12496283
7991 9818 0 None -50 2 Human 2.9 pEC50 = 2.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 102 3 1 1 1.3 CCCCC(=O)O 12496283
CHEMBL268736 9818 0 None -50 2 Human 2.9 pEC50 = 2.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 102 3 1 1 1.3 CCCCC(=O)O 12496283
DB02406 9818 0 None -50 2 Human 2.9 pEC50 = 2.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 102 3 1 1 1.3 CCCCC(=O)O 12496283
1059 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12496283
1059 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12684041
1059 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12711604
1059 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 21220428
264 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12496283
264 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12684041
264 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12711604
264 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 21220428
CHEMBL14227 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12496283
CHEMBL14227 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12684041
CHEMBL14227 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12711604
CHEMBL14227 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 21220428
DB03568 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12496283
DB03568 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12684041
DB03568 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12711604
DB03568 7537 81 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 21220428
125468 8883 0 None - 1 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 100 1 1 1 1.0 C/C(=C\C)/C(=O)O 21220428
6499 8883 0 None - 1 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 100 1 1 1 1.0 C/C(=C\C)/C(=O)O 21220428
CHEMBL52416 8883 0 None - 1 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 100 1 1 1 1.0 C/C(=C\C)/C(=O)O 21220428
1058 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12496283
1058 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12684041
1058 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12711604
1058 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 21220428
176 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12496283
176 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12684041
176 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12711604
176 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 21220428
21980959 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12496283
21980959 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12684041
21980959 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12711604
21980959 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 21220428
4211 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12496283
4211 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12684041
4211 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12711604
4211 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 21220428
CHEMBL539 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12496283
CHEMBL539 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12684041
CHEMBL539 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12711604
CHEMBL539 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 21220428
DB03166 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12496283
DB03166 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12684041
DB03166 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12711604
DB03166 7042 85 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 21220428
1032 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12496283
1032 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12684041
1032 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12711604
1032 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 21220428
1062 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12496283
1062 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12684041
1062 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12711604
1062 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 21220428
CHEMBL14021 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12496283
CHEMBL14021 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12684041
CHEMBL14021 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12711604
CHEMBL14021 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 21220428
DB03766 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12496283
DB03766 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12684041
DB03766 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12711604
DB03766 9959 78 None -8 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 21220428
5803 7182 21 None -2 2 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 18818303
5803 7182 21 None -2 2 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 21498659
854189 7182 21 None -2 2 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 18818303
854189 7182 21 None -2 2 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 21498659
CHEMBL594671 7182 21 None -2 2 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 18818303
CHEMBL594671 7182 21 None -2 2 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 294 4 1 3 4.2 CC([C@H](C(=O)Nc1nccs1)c1ccc(cc1)Cl)C 21498659
3420 10221 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 312 4 1 3 4.3 CC([C@H](C(=O)Nc1ncc(s1)F)c1ccc(cc1)Cl)C 18818303
3420 10221 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 312 4 1 3 4.3 CC([C@H](C(=O)Nc1ncc(s1)F)c1ccc(cc1)Cl)C 23066016
46226252 10221 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 312 4 1 3 4.3 CC([C@H](C(=O)Nc1ncc(s1)F)c1ccc(cc1)Cl)C 18818303
46226252 10221 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 312 4 1 3 4.3 CC([C@H](C(=O)Nc1ncc(s1)F)c1ccc(cc1)Cl)C 23066016
CHEMBL594525 10221 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 312 4 1 3 4.3 CC([C@H](C(=O)Nc1ncc(s1)F)c1ccc(cc1)Cl)C 18818303
CHEMBL594525 10221 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 312 4 1 3 4.3 CC([C@H](C(=O)Nc1ncc(s1)F)c1ccc(cc1)Cl)C 23066016
10107 10655 0 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 442 4 1 5 5.0 O=C(N1[C@H](CS[C@H]1c1ccccc1Cl)C(=O)O)c1ccc(cc1)c1c(C)noc1C 30247908
137321147 10655 0 None -1 2 Mouse 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 442 4 1 5 5.0 O=C(N1[C@H](CS[C@H]1c1ccccc1Cl)C(=O)O)c1ccc(cc1)c1c(C)noc1C 30247908
6488 7803 0 None - 1 Rat 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 4 5.9 OC(=O)CC(C(=O)N(c1scc(n1)c1cc(Cl)ccc1Cl)C1CC1)Cc1ccccc1 23589301
67209274 7803 0 None - 1 Rat 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 474 8 1 4 5.9 OC(=O)CC(C(=O)N(c1scc(n1)c1cc(Cl)ccc1Cl)C1CC1)Cc1ccccc1 23589301
1060 8870 74 None -11 3 Human 3.5 pEC50 None 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 1 1 1 0.7 CC(C(=O)O)C 12711604
6590 8870 74 None -11 3 Human 3.5 pEC50 None 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 1 1 1 0.7 CC(C(=O)O)C 12711604
CHEMBL108778 8870 74 None -11 3 Human 3.5 pEC50 None 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 1 1 1 0.7 CC(C(=O)O)C 12711604
DB02531 8870 74 None -11 3 Human 3.5 pEC50 None 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 1 1 1 0.7 CC(C(=O)O)C 12711604
12861 7982 26 None - 1 Human 6.2 pIC50 = 6.2 Functional
Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2
Guide to Pharmacology 384 4 1 3 6.2 CC(C)(C)[C@@H](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 20005104
46226294 7982 26 None - 1 Human 6.2 pIC50 = 6.2 Functional
Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2
Guide to Pharmacology 384 4 1 3 6.2 CC(C)(C)[C@@H](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 20005104
CHEMBL607315 7982 26 None - 1 Human 6.2 pIC50 = 6.2 Functional
Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2
Guide to Pharmacology 384 4 1 3 6.2 CC(C)(C)[C@@H](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 20005104
57520598 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.
Guide to Pharmacology 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 25380412
57520598 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.
Guide to Pharmacology 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 26852904
8417 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.
Guide to Pharmacology 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 25380412
8417 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.
Guide to Pharmacology 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 26852904
CHEMBL3353541 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.
Guide to Pharmacology 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 25380412
CHEMBL3353541 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.
Guide to Pharmacology 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 26852904
DB15406 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.
Guide to Pharmacology 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 25380412
DB15406 8593 33 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.Inhibition of sodium acetate-induced calcium flux <i>via</i> the FFA2 receptor.
Guide to Pharmacology 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 26852904
12655 10656 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Measuring antagonism of agonist-induced GTP&gamma;S incorporation by liquid scintillation spectroscopy.Measuring antagonism of agonist-induced GTP&gamma;S incorporation by liquid scintillation spectroscopy.
Guide to Pharmacology 419 8 2 5 2.7 O=C(N[C@H](CC1=NN=NN1)CC2=CC=C(C(F)(F)F)C=C2)CC3=CC(OC)=CC=C3 None
168433292 10656 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Measuring antagonism of agonist-induced GTP&gamma;S incorporation by liquid scintillation spectroscopy.Measuring antagonism of agonist-induced GTP&gamma;S incorporation by liquid scintillation spectroscopy.
Guide to Pharmacology 419 8 2 5 2.7 O=C(N[C@H](CC1=NN=NN1)CC2=CC=C(C(F)(F)F)C=C2)CC3=CC(OC)=CC=C3 None
12655 10656 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Measuring inhibition of sodium propionate-induced intracellular calcium flux by TR-FRET.Measuring inhibition of sodium propionate-induced intracellular calcium flux by TR-FRET.
Guide to Pharmacology 419 8 2 5 2.7 O=C(N[C@H](CC1=NN=NN1)CC2=CC=C(C(F)(F)F)C=C2)CC3=CC(OC)=CC=C3 None
168433292 10656 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Measuring inhibition of sodium propionate-induced intracellular calcium flux by TR-FRET.Measuring inhibition of sodium propionate-induced intracellular calcium flux by TR-FRET.
Guide to Pharmacology 419 8 2 5 2.7 O=C(N[C@H](CC1=NN=NN1)CC2=CC=C(C(F)(F)F)C=C2)CC3=CC(OC)=CC=C3 None
53308747 7597 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 7 2 2 4.1 OC(=O)C[C@@H](NC(=O)Cc1cccc(c1)Cl)Cc1ccc(cc1)C(F)(F)F 23066016
6487 7597 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 7 2 2 4.1 OC(=O)C[C@@H](NC(=O)Cc1cccc(c1)Cl)Cc1ccc(cc1)C(F)(F)F 23066016


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

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

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

 Mol
weight		 Rot
Bonds		 H don

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 DOI
CHEMBL5275861 200651 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 286 4 2 4 2.1 O=c1cc(CCCCCl)c2c(=O)[nH]c(=S)[nH]c2o1 10.1039/d2md00076h
137633536 163074 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Agonist activity at human FFA2 receptor by FLIPR assayAgonist activity at human FFA2 receptor by FLIPR assay
ChEMBL 368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C 10.1016/j.bmcl.2017.01.034
CHEMBL4065397 163074 0 None - 0 Human 4.6 pEC50 = 4.6 Binding
Agonist activity at human FFA2 receptor by FLIPR assayAgonist activity at human FFA2 receptor by FLIPR assay
ChEMBL 368 7 1 3 4.6 COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C 10.1016/j.bmcl.2017.01.034
CHEMBL5284951 201052 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 270 4 2 4 0.7 O=c1[nH]c(=O)c2c(CCCCCl)cc(=O)oc2[nH]1 10.1039/d2md00076h
CHEMBL5270112 200399 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assayAgonist activity at FFA2 (unknown origin) expressed in human Flp-In-293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by Lance cAMP assay
ChEMBL 252 3 2 4 1.9 CCCCc1cc(=O)oc2[nH]c(=S)[nH]c(=O)c12 10.1039/d2md00076h
57520598 8593 33 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometryAntagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometry
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/jm5012885
8417 8593 33 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometryAntagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometry
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/jm5012885
CHEMBL3353541 8593 33 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometryAntagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometry
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/jm5012885
DB15406 8593 33 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometryAntagonist activity against FFA2 receptor in human whole blood assessed as inhibition of sodium acetate-induced CD11b[AE] expression by flow cytometry
ChEMBL 484 8 1 4 5.1 OC(=O)CCCN(C(=O)[C@@]1(C)CCN1C(=O)c1csc2c1cccc2)Cc1cccc(c1)Cl 10.1021/jm5012885
145951537 169488 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 537 10 1 7 6.0 COc1ccc(-c2ccc(Cl)cc2-c2csc(N(C(=O)[C@@H](CC(=O)O)Cc3ccco3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
CHEMBL4170829 169488 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 537 10 1 7 6.0 COc1ccc(-c2ccc(Cl)cc2-c2csc(N(C(=O)[C@@H](CC(=O)O)Cc3ccco3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
145957346 168749 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 419 5 1 4 4.7 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4159019 168749 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 419 5 1 4 4.7 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
67209751 168948 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 505 10 1 6 6.0 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC3CCCC3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
CHEMBL4162307 168948 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 505 10 1 6 6.0 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC3CCCC3)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
117898644 169876 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 515 10 1 7 5.7 CC(C)C[C@H](CC(=O)O)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4177037 169876 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 515 10 1 7 5.7 CC(C)C[C@H](CC(=O)O)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
53302677 169626 1 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 474 8 1 4 5.9 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4172928 169626 1 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 474 8 1 4 5.9 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2cc(Cl)ccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
67209297 169577 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 422 7 1 5 4.3 CN(C(=O)[C@@H](CC(=O)O)CC1CCOCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4172349 169577 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 422 7 1 5 4.3 CN(C(=O)[C@@H](CC(=O)O)CC1CCOCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
138319694 169853 30 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 442 4 1 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4176503 169853 30 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 442 4 1 5 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
117898634 169174 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 479 10 1 6 5.5 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC(C)C)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
CHEMBL4165748 169174 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 479 10 1 6 5.5 COc1ccc(-c2ccccc2-c2csc(N(C(=O)[C@@H](CC(=O)O)CC(C)C)C3CC3)n2)cn1 10.1016/j.bmc.2018.09.015
67209218 169659 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 406 7 1 4 5.1 CN(C(=O)[C@@H](CC(=O)O)CC1CCCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4173387 169659 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 406 7 1 4 5.1 CN(C(=O)[C@@H](CC(=O)O)CC1CCCC1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
145951986 169483 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4170748 169483 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 453 5 1 4 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CS[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
145953670 169341 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 424 4 1 4 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4168456 169341 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 424 4 1 4 5.0 Cc1noc(C)c1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
67210172 169237 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 440 8 1 4 5.3 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2ccccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4166818 169237 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 440 8 1 4 5.3 O=C(O)C[C@@H](Cc1ccccc1)C(=O)N(c1nc(-c2ccccc2Cl)cs1)C1CC1 10.1016/j.bmc.2018.09.015
67258265 169507 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 435 5 1 3 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4171128 169507 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 435 5 1 3 5.4 COc1ccccc1-c1ccc(C(=O)N2[C@H](C(=O)O)CC[C@@H]2c2ccccc2Cl)cc1 10.1021/acs.jmedchem.8b00855
117898651 169672 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 541 10 1 7 6.2 O=C(O)C[C@@H](CC1CCCC1)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
CHEMBL4173663 169672 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 541 10 1 7 6.2 O=C(O)C[C@@H](CC1CCCC1)C(=O)N(c1nc(-c2ccccc2-c2ccc(-n3cccn3)nc2)cs1)C1CC1 10.1016/j.bmc.2018.09.015
46235794 169714 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 414 7 1 4 4.8 CN(C(=O)[C@@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
CHEMBL4174307 169714 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting methodDisplacement of [3H]ES227703 from human FFA2R expressed in CHOK1 cells after 60 mins by TopCount scintillation counting method
ChEMBL 414 7 1 4 4.8 CN(C(=O)[C@@H](CC(=O)O)Cc1ccccc1)c1nc(-c2ccccc2Cl)cs1 10.1016/j.bmc.2018.09.015
145953626 169290 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 423 4 1 3 5.3 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
CHEMBL4167577 169290 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometryDisplacement of [3H]-GLPG0974 from human FFA2 expressed in Flp-InT-REx 293 cell membranes after 2 hrs by liquid scintillation spectrometry
ChEMBL 423 4 1 3 5.3 O=C(O)[C@@H]1CS[C@H](c2ccccc2Cl)N1C(=O)c1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.8b00855
10107 10655 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for hFFA2.Binding affinity for hFFA2.
Guide to Pharmacology 442 4 1 5 5.0 O=C(N1[C@H](CS[C@H]1c1ccccc1Cl)C(=O)O)c1ccc(cc1)c1c(C)noc1C 30247908
137321147 10655 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for hFFA2.Binding affinity for hFFA2.
Guide to Pharmacology 442 4 1 5 5.0 O=C(N1[C@H](CS[C@H]1c1ccccc1Cl)C(=O)O)c1ccc(cc1)c1c(C)noc1C 30247908