Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
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(Potency)
# tested GPCRs
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(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
5803 390 15 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 390 15 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 390 15 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 162373 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 162373 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 161608 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 161608 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 162535 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 162535 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 161949 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 161949 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 161918 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 161918 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 162000 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 162000 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 181793 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 181793 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 1774 27 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 1774 27 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 1774 27 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 1774 27 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 162147 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 162147 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 162285 0 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 162285 0 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 162166 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 162166 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 161647 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 161647 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 161833 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 161833 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 162559 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 162559 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 162559 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 162559 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 162076 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 162076 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 162285 0 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 162285 0 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 162411 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 162411 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 162076 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 162076 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 162000 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 162000 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 390 15 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 390 15 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 390 15 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 161896 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 161896 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 162318 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 162318 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 162236 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 162236 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 162301 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 162301 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 162204 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 162204 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 162378 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 162378 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 161931 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 161931 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 162236 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 162236 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 162285 0 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 162285 0 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 162068 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 162068 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 162436 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 162436 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 162013 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 162013 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 161809 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 161809 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 162378 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 162378 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 161491 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 161491 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 162301 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 162301 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 161439 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 161439 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 162411 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 162411 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 162142 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 162142 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 161608 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 161608 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 161833 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 161833 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 162331 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 162331 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 162535 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 162535 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
1032 3124 71 None -13 2 Human 3.6 pEC50 = 3.6 Functional
Agonist activity at human GPCR43 transfected in HEK293 cells assessed as [35S]GTPgammaS binding by scintillation counting methodAgonist activity at human GPCR43 transfected in HEK293 cells assessed as [35S]GTPgammaS binding by scintillation counting method
ChEMBL 74 1 1 1 0.5 CCC(=O)O 10.1021/acs.jmedchem.7b00244
1062 3124 71 None -13 2 Human 3.6 pEC50 = 3.6 Functional
Agonist activity at human GPCR43 transfected in HEK293 cells assessed as [35S]GTPgammaS binding by scintillation counting methodAgonist activity at human GPCR43 transfected in HEK293 cells assessed as [35S]GTPgammaS binding by scintillation counting method
ChEMBL 74 1 1 1 0.5 CCC(=O)O 10.1021/acs.jmedchem.7b00244
CHEMBL14021 3124 71 None -13 2 Human 3.6 pEC50 = 3.6 Functional
Agonist activity at human GPCR43 transfected in HEK293 cells assessed as [35S]GTPgammaS binding by scintillation counting methodAgonist activity at human GPCR43 transfected in HEK293 cells assessed as [35S]GTPgammaS binding by scintillation counting method
ChEMBL 74 1 1 1 0.5 CCC(=O)O 10.1021/acs.jmedchem.7b00244
DB03766 3124 71 None -13 2 Human 3.6 pEC50 = 3.6 Functional
Agonist activity at human GPCR43 transfected in HEK293 cells assessed as [35S]GTPgammaS binding by scintillation counting methodAgonist activity at human GPCR43 transfected in HEK293 cells assessed as [35S]GTPgammaS binding by scintillation counting method
ChEMBL 74 1 1 1 0.5 CCC(=O)O 10.1021/acs.jmedchem.7b00244
46235794 162373 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 162373 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 162142 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 162142 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 162438 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 162438 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 161931 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 161931 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 161409 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 161409 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 161896 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 161896 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 162318 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 162318 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 162155 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 162155 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 161918 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 161918 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 161439 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 161439 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 161543 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 161543 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 162512 23 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 162512 23 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 162219 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 162219 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 162438 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 162438 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 390 15 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 390 15 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 390 15 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 162219 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 162219 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 161491 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 161491 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 161775 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 161775 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 162159 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 162159 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 162147 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 162147 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 162285 0 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 162285 0 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 162512 23 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 162512 23 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 162166 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 162166 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 162436 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 162436 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 161647 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 161647 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 161555 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 161555 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 162512 23 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 162512 23 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 162331 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 162331 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 162155 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 162155 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 162512 23 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 162512 23 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 179382 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 179382 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 162068 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 162068 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 161949 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 161949 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 162204 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 162204 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 161555 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 161555 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 162159 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 162159 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 161775 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 161775 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 161409 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 161409 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 161809 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 161809 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 200625 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 200625 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 115012 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 115012 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 115017 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 115017 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 115018 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 115018 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 198077 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 198077 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 198078 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 198078 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 198226 11 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 198226 11 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 198220 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 198220 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 198223 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 198223 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 200373 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 200373 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 198428 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 198428 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 115118 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 115118 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 115124 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 115124 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 115145 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 115145 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 115116 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 115116 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 198263 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 198263 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 200050 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 200050 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 198190 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 198190 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 115084 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 115084 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 115088 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 115088 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 115125 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 115125 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 200498 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 200498 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 115146 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 115146 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 198222 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 198222 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 198373 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 198373 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 115113 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 115113 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 115086 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 115086 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 115013 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 115013 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 115011 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 115011 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 200464 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 200464 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 200536 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 200536 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 200537 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 200537 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 200800 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 200800 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 115135 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 115135 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 115091 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 115091 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 115090 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 115090 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 198219 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 198219 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 199594 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 199594 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 198303 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 198303 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 132927 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 132927 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 200428 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 200428 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 115130 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 115130 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 200701 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 200701 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 198232 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 198232 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 198083 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 198083 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 198176 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 198176 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 198233 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 198233 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 197990 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 197990 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 198058 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 198058 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 197989 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 197989 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 132928 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 132928 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 198029 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 198029 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 198178 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 198178 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 115098 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 115098 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 115085 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 115085 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 115122 0 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 115122 0 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 198030 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 198030 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 198115 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 198115 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 115121 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 115121 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 115143 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 115143 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 115102 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 115102 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 115014 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 115014 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 115103 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 115103 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 115129 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 115129 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 200535 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 200535 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 115105 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 115105 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 115126 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 115126 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 115000 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 115000 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 115016 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 115016 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 115110 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 115110 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 115114 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 115114 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 115132 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 115132 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 115096 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 115096 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 200499 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 200499 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 115120 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 115120 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 115104 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 115104 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 115140 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 115140 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 200337 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 200337 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 115087 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 115087 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 198177 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 198177 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 115094 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 115094 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 115141 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 115141 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 115106 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 115106 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 115097 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 115097 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 200700 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 200700 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 115101 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 115101 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 115089 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 115089 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 115111 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 115111 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 198184 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 198184 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 198227 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 198227 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 115093 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 115093 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 115015 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 115015 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 115139 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 115139 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 198221 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 198221 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 3379 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 3379 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 3379 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 198225 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 198225 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 115138 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 115138 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 198257 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 198257 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 200538 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 200538 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 200892 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 200892 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 115115 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 115115 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 115117 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 115117 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 115112 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 115112 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 115092 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 115092 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 200579 5 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 200579 5 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 198020 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 198020 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 198228 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 198228 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 115131 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 115131 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 198027 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 198027 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 115137 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 115137 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 200847 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 200847 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 198488 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 198488 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 115127 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 115127 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 115109 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 115109 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 200372 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 200372 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 115119 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 115119 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 115123 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 115123 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 115128 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 115128 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 390 15 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 390 15 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 390 15 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
46226275 198017 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 198017 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
46226294 200180 20 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](C(=O)Nc1ncc(-c2ccccc2)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
CHEMBL607315 200180 20 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](C(=O)Nc1ncc(-c2ccccc2)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226273 200798 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 200798 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 200799 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 200799 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 200242 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 200242 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 115136 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 115136 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 115095 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 115095 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 115099 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 115099 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 115108 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 115108 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 115134 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 115134 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 115107 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 115107 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 198110 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 198110 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 198124 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 198124 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 198182 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 198182 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 200645 43 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 200645 43 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 198064 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 198064 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 115133 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 115133 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 198265 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 198265 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 198151 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 198151 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 1774 27 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 1774 27 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 1774 27 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 1774 27 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 115144 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 115144 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 115142 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 115142 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 252 80 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
176 252 80 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
21980959 252 80 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
4211 252 80 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
CHEMBL539 252 80 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
DB03166 252 80 None 3 2 Human 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 60 0 1 1 0.1 CC(=O)O None
10107 3808 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 3808 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 3808 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 3808 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 35 109 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 35 109 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 35 109 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 2983 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 2983 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 2983 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 2983 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 737 75 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 737 75 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 737 75 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 737 75 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 21220428
264 737 75 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12496283
264 737 75 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12684041
264 737 75 None -7 3 Human 3.8 pEC50 = 3.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 88 2 1 1 0.9 CCCC(=O)O 12711604
264 737 75 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 737 75 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 737 75 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 737 75 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 737 75 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 737 75 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 737 75 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 737 75 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 737 75 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 2062 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 2062 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 2062 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 252 80 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 252 80 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 252 80 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 252 80 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 21220428
176 252 80 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12496283
176 252 80 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12684041
176 252 80 None 3 2 Human 3.9 pEC50 = 3.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 60 0 1 1 0.1 CC(=O)O 12711604
176 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 252 80 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 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12496283
1032 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12684041
1032 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12711604
1032 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 21220428
1062 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12496283
1062 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12684041
1062 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12711604
1062 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 21220428
CHEMBL14021 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12496283
CHEMBL14021 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12684041
CHEMBL14021 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12711604
CHEMBL14021 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 21220428
DB03766 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12496283
DB03766 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12684041
DB03766 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 12711604
DB03766 3124 71 None -13 2 Human 4.0 pEC50 = 4.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 74 1 1 1 0.5 CCC(=O)O 21220428
5803 390 15 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 390 15 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 390 15 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 390 15 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 390 15 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 390 15 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 3379 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 3379 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 3379 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 3379 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 3379 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 3379 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 3808 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 3808 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 999 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 999 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 2050 69 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 2050 69 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 2050 69 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 2050 69 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
57520598 1774 27 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 1774 27 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 1774 27 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 1774 27 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 1774 27 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 1774 27 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 1774 27 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 1774 27 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 3809 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 3809 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 795 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 795 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




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
137633536 155742 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 155742 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
57520598 1774 27 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 1774 27 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 1774 27 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 1774 27 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 162147 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 162147 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 161409 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 161409 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 161608 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 161608 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 162535 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 162535 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 162285 0 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 162285 0 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 162236 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 162236 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 162512 23 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 162512 23 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 161833 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 161833 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 162318 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 162318 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 162142 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 162142 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 162000 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 162000 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 161896 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 161896 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 162166 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 162166 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 162331 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 162331 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 162373 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 162373 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 161949 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 161949 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 3808 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 3808 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