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
(Potency)
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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 162385 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 162385 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 161620 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 161620 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 162547 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 162547 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 161961 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 161961 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 161930 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 161930 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 162012 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 162012 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 181803 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 181803 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 1782 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 1782 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 1782 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 1782 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 162159 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 162159 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 162297 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 162297 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 162178 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 162178 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 161659 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 161659 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 161845 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 161845 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 162571 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 162571 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 162571 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 162571 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 162088 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 162088 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 162297 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 162297 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 162423 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 162423 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 162088 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 162088 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 162012 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 162012 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 161908 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 161908 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 162330 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 162330 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 162248 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 162248 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 162313 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 162313 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 162216 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 162216 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 162390 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 162390 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 161943 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 161943 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 162248 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 162248 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 162297 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 162297 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 162080 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 162080 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 162448 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 162448 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 162025 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 162025 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 161821 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 161821 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 162390 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 162390 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 161503 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 161503 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 162313 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 162313 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 161451 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 161451 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 162423 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 162423 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 162154 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 162154 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 161620 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 161620 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 161845 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 161845 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 162343 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 162343 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 162547 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 162547 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 3136 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 3136 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 3136 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 3136 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 162385 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 162385 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 162154 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 162154 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 162450 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 162450 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 161943 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 161943 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 161421 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 161421 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 161908 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 161908 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 162330 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 162330 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 162167 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 162167 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 161930 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 161930 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 161451 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 161451 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 161555 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 161555 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 162524 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 162524 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 162231 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 162231 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 162450 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 162450 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 162231 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 162231 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 161503 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 161503 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 161787 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 161787 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 162171 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 162171 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 162159 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 162159 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 162297 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 162297 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 162524 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 162524 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 162178 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 162178 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 162448 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 162448 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 161659 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 161659 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 161567 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 161567 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 162524 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 162524 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 162343 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 162343 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 162167 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 162167 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 162524 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 162524 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 179392 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 179392 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 162080 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 162080 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 161961 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 161961 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 162216 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 162216 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 161567 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 161567 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 162171 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 162171 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 161787 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 161787 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 161421 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 161421 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 161821 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 161821 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 200634 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 200634 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 115025 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 115025 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 115030 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 115030 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 115031 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 115031 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 198087 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 198087 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 198088 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 198088 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 198236 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 198236 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 198230 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 198230 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 198233 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 198233 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 200382 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 200382 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 198438 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 198438 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 115131 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 115131 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 115137 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 115137 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 115158 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 115158 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 115129 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 115129 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 198273 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 198273 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 200060 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 200060 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 198200 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 198200 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 115097 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 115097 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 115101 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 115101 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 115138 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 115138 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 200507 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 200507 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 115159 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 115159 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 198232 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 198232 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 198383 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 198383 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 115126 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 115126 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 115099 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 115099 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 115026 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 115026 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 115024 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 115024 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 200473 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 200473 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 200545 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 200545 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 200546 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 200546 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 200809 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 200809 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 115148 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 115148 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 115104 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 115104 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 115103 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 115103 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 198229 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 198229 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 199604 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 199604 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 198313 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 198313 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 132940 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 132940 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 200437 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 200437 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 115143 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 115143 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 200710 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 200710 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 198242 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 198242 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 198093 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 198093 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 198186 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 198186 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 198243 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 198243 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 198000 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 198000 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 198068 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 198068 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 197999 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 197999 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 132941 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 132941 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 198039 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 198039 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 198188 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 198188 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 115111 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 115111 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 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 451 6 0 4 4.6 CC1(C(=O)N(CC#N)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
CHEMBL3353465 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 451 6 0 4 4.6 CC1(C(=O)N(CC#N)Cc2ccc(Cl)cc2)CCN1C(=O)Cc1csc2ccccc12 10.1021/jm5012885
70559604 115135 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 115135 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 198040 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 198040 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 198125 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 198125 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 115134 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 115134 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 115156 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 115156 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 115115 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 115115 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 115027 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 115027 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 115116 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 115116 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 115142 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 115142 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 200544 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 200544 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 115118 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 115118 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 115139 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 115139 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 115013 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 115013 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 115029 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 115029 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 115123 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 115123 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 115127 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 115127 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 115145 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 115145 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 115109 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 115109 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 200508 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 200508 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 115133 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 115133 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 115117 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 115117 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 115153 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 115153 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 200346 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 200346 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 115100 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 115100 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 198187 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 198187 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 115107 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 115107 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 115154 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 115154 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 115119 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 115119 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 115110 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 115110 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 200709 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 200709 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 115114 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 115114 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 115102 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 115102 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 115124 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 115124 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 198194 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 198194 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 198237 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 198237 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 115106 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 115106 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 115028 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 115028 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 115152 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 115152 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 198231 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 198231 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 3392 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 3392 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 3392 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 198235 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 198235 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 115151 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 115151 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 198267 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 198267 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 200547 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 200547 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 200901 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 200901 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 115128 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 115128 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 115130 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 115130 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 115125 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 115125 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 115105 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 115105 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 200588 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 200588 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 198030 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 198030 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 198238 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 198238 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 115144 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 115144 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 198037 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 198037 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 115150 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 115150 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 200856 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 200856 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 198498 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 198498 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 115140 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 115140 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 115122 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 115122 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 200381 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 200381 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 115132 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 115132 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 115136 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 115136 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 115141 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 115141 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
12861 1176 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](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 10.1016/j.bmcl.2009.11.112
46226294 1176 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](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 10.1016/j.bmcl.2009.11.112
CHEMBL607315 1176 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](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 10.1016/j.bmcl.2009.11.112
46226275 198027 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 198027 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP productionAgonist activity at human FFA2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production
ChEMBL 386 3 1 3 5.3 CC(C)(C)[C@H](C(=O)Nc1ncc(Br)s1)c1ccc(Cl)cc1 10.1016/j.bmcl.2009.11.112
46226273 200807 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 200807 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 200808 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 200808 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 200251 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 200251 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 115149 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 115149 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 115108 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 115108 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 115112 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 115112 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 115121 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 115121 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 115147 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 115147 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 115120 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 115120 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 198120 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 198120 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 198134 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 198134 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 198192 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 198192 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 200654 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 200654 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 198074 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 198074 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 115146 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 115146 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 198275 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 198275 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 198161 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 198161 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 1782 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 1782 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 1782 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 1782 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 115157 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 115157 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 115155 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 115155 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 3820 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 3820 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 3820 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 3820 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 2995 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 2995 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 2995 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 2995 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 739 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 739 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 739 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 739 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
264 739 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
264 739 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
264 739 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
264 739 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 739 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 739 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 739 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 739 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 739 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 739 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 739 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 739 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 2071 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 2071 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 2071 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3136 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 3392 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 3392 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 3392 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 3392 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 3392 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 3392 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 3820 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 3820 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 1001 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 1001 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 2058 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 2058 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 2058 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 2058 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
12861 1176 20 None - 1 Human 6.2 pIC50 = 6.2 Functional
Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2
Guide to Pharmacology 384 4 1 3 6.2 CC(C)(C)[C@@H](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 20005104
46226294 1176 20 None - 1 Human 6.2 pIC50 = 6.2 Functional
Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2
Guide to Pharmacology 384 4 1 3 6.2 CC(C)(C)[C@@H](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 20005104
CHEMBL607315 1176 20 None - 1 Human 6.2 pIC50 = 6.2 Functional
Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2Determined in a cAMP assay measuring inhibition of forskolin-induced cAMP response in CHO cells expressing hFFA2
Guide to Pharmacology 384 4 1 3 6.2 CC(C)(C)[C@@H](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=C(S2)C3=CC=CC=C3 20005104
57520598 1782 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 1782 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 1782 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 1782 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 1782 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 1782 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 1782 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 1782 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 3821 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Measuring antagonism of agonist-induced GTP&gamma;S incorporation by liquid scintillation spectroscopy.Measuring antagonism of agonist-induced GTP&gamma;S incorporation by liquid scintillation spectroscopy.
Guide to Pharmacology 419 8 2 5 2.7 O=C(N[C@H](CC1=NN=NN1)CC2=CC=C(C(F)(F)F)C=C2)CC3=CC(OC)=CC=C3 None
168433292 3821 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 3821 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Measuring inhibition of sodium propionate-induced intracellular calcium flux by TR-FRET.Measuring inhibition of sodium propionate-induced intracellular calcium flux by TR-FRET.
Guide to Pharmacology 419 8 2 5 2.7 O=C(N[C@H](CC1=NN=NN1)CC2=CC=C(C(F)(F)F)C=C2)CC3=CC(OC)=CC=C3 None
168433292 3821 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 797 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 797 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 155754 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 155754 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 1782 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 1782 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 1782 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 1782 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 162159 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 162159 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 161421 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 161421 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 161620 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 161620 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 162547 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 162547 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 162297 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 162297 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 162248 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 162248 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 162524 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 162524 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 161845 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 161845 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 162330 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 162330 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 162154 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 162154 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 162012 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 162012 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 161908 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 161908 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 162178 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 162178 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 162343 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 162343 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 162385 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 162385 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 161961 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 161961 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 3820 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 3820 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